Drug/Small Molecule:
tacrolimus

last updated 08/10/2011

Dutch Pharmacogenetics Working Group Guideline for tacrolimus and CYP3A5

Summary

There is evidence to support an interaction between tacrolimus and CYP3A5, however, there are no dosing recommendations at this time.

Annotation

The Royal Dutch Pharmacists Association - Pharmacogenetics Working Group has evaluated therapeutic dose recommendations for tacrolimus based on CYP3A5 genotype [Article:21412232]. They found evidence to support an interaction between tacrolimus and CYP3A5. However, they make no dosing recommendations at this time, due to fact that "in Dutch transplantation hospitals the tacrolimus dose is titrated in response to therapeutic drug monitoring."

Genotype Therapeutic Dose Recommendation Level of Evidence Clinical Relevance
CYP3A5 *1/*1 None Published controlled studies of good quality* relating to phenotyped and/or genotyped patients or healthy volunteers, and having relevant pharmacokinetic or clinical endpoints. Clinical effect (S): short-lived discomfort (< 48 hr) without permanent injury: e.g. reduced decrease in resting heart rate; reduction in exercise tachycardia; decreased pain relief from oxycodone; ADE resulting from increased bioavailability of atomoxetine (decreased appetite, insomnia, sleep disturbance etc); neutropenia > 1.5x109/l; leucopenia > 3.0x109/l; thrombocytopenia > 75x109/l; moderate diarrhea not affecting daily activities; reduced glucose increase following oral glucose tolerance test.
CYP3A5 *1/*3 None Published controlled studies of good quality* relating to phenotyped and/or genotyped patients or healthy volunteers, and having relevant pharmacokinetic or clinical endpoints. Clinical effect (S): long-standing discomfort (> 168 hr), permanent symptom or invalidating injury e.g. failure of prophylaxis of atrial fibrillation; venous thromboembolism; decreased effect of clopidogrel on inhibition of platelet aggregation; ADE resulting from increased bioavailability of phenytoin; INR > 6.0; neutropenia 0.5-1.0x109/l; leucopenia 1.0-2.0x109/l; thrombocytopenia 25-50x109/l; severe diarrhea.

PharmGKB has no annotated drug labels with pharmacogenomic information for this drug/small molecule. If you know of a drug label with PGx, send us a message.

Links to Unannotated Labels

These links are to labels associated with tacrolimus that have not been annotated by PharmGKB.

  1. DailyMed - DrugLabel PA166105255

Clinical Variants that meet the highest level of criteria, manually curated by PharmGKB, are shown below.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all tacrolimus variant annotations

Gene ? Variant?
(142)
Alternate Names ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available CA VA CYP2C19 *1 N/A N/A N/A
No VIP available CA VA CYP2C19 *2 N/A N/A N/A
No VIP available No VIP available VA CYP2C8 *1A N/A N/A N/A
No VIP available No VIP available VA CYP2C8 *3 N/A N/A N/A
No VIP available CA VA CYP3A4 *1 N/A N/A N/A
No VIP available No VIP available VA CYP3A4 *1B N/A N/A N/A
No VIP available CA VA CYP3A4 *1G N/A N/A N/A
No VIP available No VIP available VA CYP3A4 *18B N/A N/A N/A
No VIP available No VIP available VA CYP3A4 *22 N/A N/A N/A
No VIP available No VIP available VA CYP3A5 *1A N/A N/A N/A
No VIP available No VIP available VA CYP3A5 *3A N/A N/A N/A
No VIP available No VIP available VA CYP3A5 *6 N/A N/A N/A
No VIP available No VIP available VA CYP3A5 *7 N/A N/A N/A
No VIP available CA VA
rs10264272 1226G>A, 1245G>A, 19787G>A, 37295678C>T, 624G>A, 867G>A, 975G>A, 986G>A, 99262835C>T, CYP3A5*6, CYP3A5:711G>A, CYP3A5:Lys208Lys, Lys208=
C > T
Not Available
Lys208Lys
No VIP available CA VA
rs1042597 234526871C>G, 234526871C>T, 33482C>G, 33482C>T, 473130C>G, 473130C>T, 518C>G, 518C>T, Ala173Gly, Ala173Val, UGT1A8*2
C > G
C > T
Missense
Ala173Val
Ala173Gly
rs1045642 208920T>A, 208920T>C, 25171488A>G, 25171488A>T, 3435T>A, 3435T>C, 87138645A>G, 87138645A>T, ABCB1*6, ABCB1: 3435C>T, ABCB1: C3435T, ABCB1: c.3435C>T, ABCB1:3435C>T, Ile1145=, Ile1145Ile, MDR1 3435C>T, MDR1 C3435T, PGP C3435T, c.3435C>T, mRNA 3853C>T
A > T
A > G
Synonymous
Ile1145Ile
No VIP available CA VA
rs1057868 13647849C>T, 1508C>T, 3514924C>T, 75587C>T, 75615006C>T, Ala503Val, POR A503V, POR*28
C > T
Missense
Ala503Val
No VIP available No Clinical Annotations available VA
rs11265572 12701705G>T, 161213063G>T
G > T
Not Available
No VIP available No Clinical Annotations available VA
rs1128503 1236T>C, 167964T>C, 25043506A>G, 87550285A>G, ABCB1 1236C>T, ABCB1*8, ABCB1: c.1236T>C, ABCB1:1236C>T, ABCB1:1236T>C, Gly412=, Gly412Gly, mRNA 1654T>C, p.Gly412Gly
A > G
Not Available
Gly412Gly
No VIP available No Clinical Annotations available VA
rs11584174 12701095C>T, 161212453C>T, 548G>A
C > T
Not Available
No VIP available No Clinical Annotations available VA
rs12333983 *1642A>T, 32695A>T, 37386957T>A, 99354114T>A
T > A
3' Flanking
No VIP available No Clinical Annotations available VA
rs15524 *14T>C, 1885T>C, 2125T>C, 3229T>C, 36708T>C, 37278757A>G, 99245914A>G
A > G
Not Available
No VIP available No Clinical Annotations available VA
rs165599 *522G>A, 19956781G>A, 3108931G>A, 32519G>A, 52529C>T
G > A
3' UTR
No VIP available No Clinical Annotations available VA
rs1799752 16457_16458insATACAGTCACTTTTTTTTTTTTTTTGAGACGGAGTCTCGCTCTGTCGCCC, 2306-119_2306-118insATACAGTCACTTTTTTTTTTTTTTTGAGACGGAGTCTCGCTCTGTCGCCC, 26840042_26840043insATACAGTCACTTTTTTTTTTTTTTTGAGACGGAGTCTCGCTCTGTCGCCC, 584-119_584-118insATACAGTCACTTTTTTTTTTTTTTTGAGACGGAGTCTCGCTCTGTCGCCC, 61565890_61565891insATACAGTCACTTTTTTTTTTTTTTTGAGACGGAGTCTCGCTCTGTCGCCC, ACE D/I
- > ATACAGTCACTTTTTTTTTTTTTTTGAGACGGAGTCTCGCTCTGTCGCCC
Intronic
No VIP available No Clinical Annotations available VA
rs1800871 -854T>C, 206946634A>G, 4206T>C, 464413A>G
A > G
5' Flanking
No VIP available No Clinical Annotations available VA
rs1800872 -627A>C, 206946407T>G, 4433A>C, 464186T>G
T > G
5' Flanking
No VIP available No Clinical Annotations available VA
rs1800896 -1117A>G, 206946897T>C, 3943A>G, 464676T>C
T > C
5' Flanking
No VIP available No Clinical Annotations available VA
rs1851426 -1232T>C, 37415779A>G, 3873T>C, 99382936A>G
A > G
5' Flanking
No VIP available CA VA
rs1927907 -340-1903C>T, 11305C>T, 120472764C>T, 140+1757C>T, 260+1757C>T, 49637296C>T
C > T
Intronic
rs2032582 186947T>A, 186947T>G, 25193461A>C, 25193461A>T, 2677A, 2677G, 2677T, 2677T>A, 2677T>G, 3095G>T/A, 87160618A>C, 87160618A>T, 893 Ala, 893 Ser, 893 Thr, ABCB1*7, ABCB1: 2677G>T/A, ABCB1: 2677T/A>G, ABCB1: A893S, ABCB1: G2677T/A, ABCB1: c.2677G>T/A, ABCB1:2677G>A/T, ABCB1:2677G>T/A, ABCB1:A893T, Ala893Ser/Thr, MDR1, MDR1 G2677T/A, Ser893Ala, Ser893Thr, mRNA 3095G>T/A, p.Ala893Ser/Thr
A > T
A > C
Missense
Ser893Ala
Ser893Thr
No VIP available CA VA
rs2066844 19877C>T, 2104C>T, 4360125C>T, 50745926C>T
C > T
Missense
Arg702Trp
No VIP available No Clinical Annotations available VA
rs2231142 13600044G>T, 32689C>A, 421C>A, 89052323G>T, ABCG2: Q141K, ABCG2:421C>A, ABCG2:Q141K, ABCG2:c.421C>A, Gln141Lys, rs2231142
G > T
Missense
Gln141Lys
No VIP available No Clinical Annotations available VA
rs2237895 1414-11803A>C, 1688-11803A>C, 1795-11803A>C, 2797194A>C, 2857194A>C, 395974A>C
A > C
Intronic
No VIP available No Clinical Annotations available VA
rs2239393 -848A>G, 139+90A>G, 19950428A>G, 26166A>G, 289+90A>G, 3102578A>G
A > G
5' Flanking
No VIP available No Clinical Annotations available VA
rs2242480 1023+12G>A, 1026+12G>A, 25343G>A, 37394309C>T, 99361466C>T
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs2257401 1226G>C, 31137C>C, 37339528C>G, 99306685C>G, Arg409Thr, CYP3A7:1226C>G, T409R
C > G
Missense
Arg409Thr
No VIP available No Clinical Annotations available VA
rs2276707 1055-17C>G, 1055-17C>T, 119534153C>G, 119534153C>T, 26029299C>G, 26029299C>T, 39823C>G, 39823C>T, 827-17C>G, 827-17C>T, 938-17C>G, 938-17C>T
C > G
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs2278293 128040752C>T, 14285G>A, 250-159G>A, 309+134G>A, 324+119G>A, 471+119G>A, 480+119G>A, 549+119G>A, 579+119G>A, 66073595C>T, IMPDH1:IVS7+125G4A
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs2278294 128040699C>T, 14338G>A, 250-106G>A, 310-106G>A, 325-106G>A, 472-106G>A, 481-106G>A, 550-106G>A, 580-106G>A, 66073542C>T, IMPDH1:IVS8-106G4A
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs2501870 12701211G>A, 161212569G>A, 432C>T
G > A
Not Available
No VIP available No Clinical Annotations available VA
rs2687116 20866G>T, 37398786C>A, 670+34G>T, 99365943C>A
C > A
Intronic
No VIP available CA VA
rs2740574 -392G>A, 37414939C>T, 4713G>A, 5'-flanking region -392A>G, 99382096C>T, CYP3A4*1B, CYP3A4-V, CYP3A4:-392A>G
C > T
5' Flanking
No VIP available CA No Variant Annotations available
rs28371759 25183T>C, 37394469A>G, 875T>C, 878T>C, 99361626A>G, CYP3A4*18, L293P, Leu292Pro, Leu293Pro
A > G
Missense
Leu293Pro
No VIP available No Clinical Annotations available VA
rs2868177 13622746A>G, 188+6405A>G, 3489821A>G, 50484A>G, 75589903A>G
A > G
Intronic
No VIP available No Clinical Annotations available VA
rs3213619 -129T>C, 117372T>C, 25263036A>G, 87230193A>G, ABCB1:T-129C
A > G
5' UTR
No VIP available CA VA
rs35599367 20493C>T, 37399159G>A, 522-191C>T, 99366316G>A, CYP3A4*22
G > A
Intronic
No VIP available CA VA
rs41303343 1035_1036insT, 1397_1398insT, 1637_1638insT, 2741_2742insT, 32228_32229insT, 37283236_37283237insA, 99250393_99250394insA, Pro345_Thr346delinsProTyrLeufs
- > A
Not Available
Thr346TyrLeu
No VIP available CA VA
rs4253728 209-1003G>A, 26000636G>A, 46610067G>A, 68569G>A
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs4646312 -1863T>C, -91-385T>C, 19948337T>C, 24075T>C, 3100487T>C
T > C
Intronic
No VIP available No Clinical Annotations available VA
rs4646437 21726C>T, 37397926G>A, 671-202C>T, 671-205C>T, 99365083G>A
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs4646457 37277923A>C, 37542T>G, 99245080A>C
A > C
Not Available
No VIP available No Clinical Annotations available VA
rs4646458 37277856T>G, 37609A>C, 99245013T>G
T > G
Not Available
No VIP available No Clinical Annotations available VA
rs4680 1-5G>A, 19951271G>A, 27009G>A, 3103421G>A, 322G>A, 472G>A, COMP: Val158Met, COMT:Val108Met, Val108Met, Val158Met
G > A
5' Flanking
Val158Met
No VIP available CA VA
rs4823613 208+3819A>G, 25988876A>G, 46598307A>G, 56809A>G
A > G
Intronic
No VIP available No Clinical Annotations available VA
rs4986910 1331T>C, 1334 C allele, 1334T>C, 28285T>C, 37391367A>G, 445Thr allele, 99358524A>G, CYP3A4*3, CYP3A4:M445T, Met444Thr, Met445Thr, mRNA 1438T>C
A > G
Missense
Met445Thr
No VIP available No Clinical Annotations available VA
rs5030952 241542703C>T, 733571C>T, SNP-63: rs5030952:C>T
C > T
Not Available
No VIP available No Clinical Annotations available VA
rs55802895 12701385C>T, 161212743C>T, 258G>A
C > T
Not Available
No VIP available No Clinical Annotations available VA
rs6267 1-1013G>T, 19950263G>T, 214G>T, 26001G>T, 3102413G>T, 64G>T, Ala22Ser, Ala72Ser, COMT: Ala72Ser
G > T
5' Flanking
Ala72Ser
No VIP available No Clinical Annotations available VA
rs6956344 1250+513G>A, 1253+513G>A, 27658G>A, 37391994C>T, 99359151C>T
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs737865 -795T>C, -92+701A>G, 19930121A>G, 3082271A>G, 4239T>C, 5859A>G
A > G
5' Flanking
rs776746 12083G>A, 219-237G>A, 321-1G>A, 37303382C>T, 581-237G>A, 689-1G>A, 99270539C>T, CYP3A5*1, CYP3A5*3, CYP3A5*3C, CYP3A5:6986A>G, g.6986A>G, intron 3 splicing defect, rs776746 A>G
C > T
Acceptor
No VIP available No Clinical Annotations available VA
rs7903146 114758349C>T, 381+46983C>T, 382-41435C>T, 450+33966C>T, 53341C>T, 65562813C>T
C > T
Intronic
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 142

Overview

Generic Names
  • FK-506
  • FK5
  • FK506
  • K506
  • Tacarolimus
  • tacrolimus
  • tacrolimus hydrate
Trade Names
  • Fujimycin
  • LCP-Tacro
  • Prograf
  • Protopic
Brand Mixture Names

PharmGKB Accession Id:
PA451578

Description

Tacrolimus (also FK-506 or Fujimycin) is an immunosuppressive drug whose main use is after organ transplant to reduce the activity of the patient's immune system and so the risk of organ rejection. It is also used in a topical preparation in the treatment of severe atopic dermatitis, severe refractory uveitis after bone marrow transplants, and the skin condition vitiligo. It was discovered in 1984 from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. Tacrolimus is chemically known as a macrolide. It reduces peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP-12 (FK506 binding protein) creating a new complex. This FKBP12-FK506 complex interacts with and inhibits calcineurin thus inhibiting both T-lymphocyte signal transduction and IL-2 transcription.

Source: Drug Bank

Indication

For use after allogenic organ transplant to reduce the activity of the patient's immune system and so the risk of organ rejection. It was first approved by the FDA in 1994 for use in liver transplantation, this has been extended to include kidney, heart, small bowel, pancreas, lung, trachea, skin, cornea, and limb transplants. It has also been used in a topical preparation in the treatment of severe atopic dermatitis.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

The mechanism of action of tacrolimus in atopic dermatitis is not known. While the following have been observed, the clinical significance of these observations in atopic dermatitis is not known. It has been demonstrated that tacrolimus inhibits T-lymphocyte activation by first binding to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is then formed and the phosphatase activity of calcineurin is inhibited. This prevents the dephosphorylation and translocation of nuclear factor of activated T-cells (NF-AT), a nuclear component thought to initiate gene transcription for the formation of lymphokines. Tacrolimus also inhibits the transcription for genes which encode IL-3, IL-4, IL-5, GM-CSF, and TNF-, all of which are involved in the early stages of T-cell activation. Additionally, tacrolimus has been shown to inhibit the release of pre-formed mediators from skin mast cells and basophils, and to downregulate the expression of FceRI on Langerhans cells.

Source: Drug Bank

Pharmacology

Tacrolimus is a macrolide antibiotic. It acts by reducing peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP-12 (FK506 binding protein) creating a new complex. This inhibits both T-lymphocyte signal transduction and IL-2 transcription. Although this activity is similar to cyclosporine studies have shown that the incidence of acute rejection is reduced by tacrolimus use over cyclosporine. Tacrolimus has also been shown to be effective in the topical treatment of eczema, particularly atopic eczema. It suppresses inflammation in a similar way to steroids, but is not as powerful. An important dermatological advantage of tacrolimus is that it can be used directly on the face; topical steroids cannot be used on the face, as they thin the skin dramatically there. On other parts of the body, topical steroid are generally a better treatment.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic, extensive, primarily by CYP3A4. The major metabolite identified in incubations with human liver microsomes is 13-demethyl tacrolimus. In in vitro studies, a 31-demethyl metabolite has been reported to have the same activity as tacrolimus.

Source: Drug Bank

Protein Binding

75-99%

Source: Drug Bank

Absorption

20% bioavailability; less after eating food rich in fat

Source: Drug Bank

Half-Life

11.3 hours (range from 3.5 to 40.6 hours)

Source: Drug Bank

Toxicity

Side effects can be severe and include blurred vision, liver and kidney problems (it is nephrotoxic), seizures, tremors, hypertension, hypomagnesemia, diabetes mellitus, hyperkalemia, itching, insomnia, confusion. LD 50=134-194 mg/kg (rat).

Source: Drug Bank

Clearance

Source: Drug Bank

Route of Elimination

In man, less than 1% of the dose administered is excreted unchanged in urine. Fecal elimination accounted for 92.6±30.7%, urinary elimination accounted for 2.3±1.1%.

Source: Drug Bank

Volume of Distribution

Source: Drug Bank

Chemical Properties

Chemical Formula

C44H69NO12

Source: Drug Bank

Isomeric SMILES

C[C@@H]1C[C@@H]([C@@H]2[C@H](C[C@H]([C@@](O2)(C(=O)C(=O)N3CCCC[C@H]3C(=O)O[C@@H]([C@@H]([C@H](CC(=O)[C@@H](/C=C(/C1)\C)CC=C)O)C)/C(=C\[C@@H]4CC[C@H]([C@@H](C4)OC)O)/C)O)C)OC)OC

Source: Drug Bank

CO[C@@H]1C[C@@H](CC[C@H]1O)\C=C(/C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@]2(O)O[C@@H]([C@H](C[C@H]2C)OC)[C@H](C[C@@H](C)C\C(C)=C\[C@@H](CC=C)C(=O)C[C@H](O)[C@H]1C)OC

Source: Drug Bank

Canonical SMILES

CO[C@@H]1C[C@@H]

Source: Drug Bank

Average Molecular Weight

804.0182

Source: Drug Bank

Monoisotopic Molecular Weight

803.481976677

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
FKBP1A (source: Drug Bank)

Drug Interactions

Drug Description
tacrolimus The protease inhibitor increase the effect and toxicity of tacrolimus (source: Drug Bank)
tacrolimus The protease inhibitor, amprenavir, increase the effect and toxicity of tacrolimus. (source: Drug Bank)
tacrolimus Increases the effect and toxicity of immunosuppressant (source: Drug Bank)
tacrolimus Increases the effect and toxicity of immunosuppressant (source: Drug Bank)
tacrolimus Tacrolimus increases the effect and toxicity of the statin (source: Drug Bank)
tacrolimus Increases tacrolimus levels (source: Drug Bank)
tacrolimus Increases tacrolimus levels (source: Drug Bank)
tacrolimus This antibiotic increases the effect and toxicity of tacrolimus (source: Drug Bank)
tacrolimus This antibiotic increases the effect and toxicity of tacrolimus (source: Drug Bank)
tacrolimus Additive toxicities for these agents (source: Drug Bank)
tacrolimus Additive toxicities for these agents (source: Drug Bank)
tacrolimus Increases the effect and toxicity of tacrolimus (source: Drug Bank)
tacrolimus Increases levels of tacrolimus (source: Drug Bank)
tacrolimus Increases levels of tacrolimus (source: Drug Bank)
tacrolimus Erythromycin increases the effect and toxicity of tacrolimus (source: Drug Bank)
tacrolimus Erythromycin increases the effect and toxicity of tacrolimus (source: Drug Bank)
tacrolimus Felodipine increases tacrolimus levels (source: Drug Bank)
tacrolimus Felodipine increases tacrolimus levels (source: Drug Bank)
tacrolimus Increases the effect of the immunosuppressant (source: Drug Bank)
tacrolimus Increases the effect of the immunosuppressant (source: Drug Bank)
tacrolimus The protease inhibitor increases the effect and toxicity of tacrolimus (source: Drug Bank)
tacrolimus The protease inhibitor, fosamprenavir, may increase the effect and toxicity of tacrolimus. (source: Drug Bank)
tacrolimus The hydantoin decreases the effect of tacrolimus (source: Drug Bank)
tacrolimus Increases the effect and toxicity of tacrolimus (source: Drug Bank)
tacrolimus Increases the effect and toxicity of tacrolimus (source: Drug Bank)
tacrolimus The imidazole increases the effect of immunosuppressant (source: Drug Bank)
tacrolimus The imidazole increases the effect of immunosuppressant (source: Drug Bank)
tacrolimus The imidazole increases the effect of immunosuppressant (source: Drug Bank)
tacrolimus The imidazole increases the effect of immunosuppressant (source: Drug Bank)
tacrolimus Tacrolimus increases the effect and toxicity of the statin (source: Drug Bank)
tacrolimus Metronidazole increases the levels/toxicity of tacrolimus (source: Drug Bank)
tacrolimus Metronidazole increases the levels/toxicity of tacrolimus (source: Drug Bank)
tacrolimus Increased mycophenolic acid levels (source: Drug Bank)
tacrolimus Increased mycophenolic acid levels (source: Drug Bank)
tacrolimus Nefazodone increases the effect and toxicity of tacrolimus (source: Drug Bank)
tacrolimus Nefazodone increases the effect and toxicity of tacrolimus (source: Drug Bank)
tacrolimus The protease inhibitor increases the effect and toxicity of tacrolimus (source: Drug Bank)
tacrolimus The protease inhibitor, nelfinavir, may increase the effect and toxicity of tacrolimus. (source: Drug Bank)
tacrolimus Nifedipine increases serum levels of tacrolimus (source: Drug Bank)
tacrolimus Nifedipine increases serum levels of tacrolimus (source: Drug Bank)
tacrolimus The hydantoin decreases the effect of tacrolimus (source: Drug Bank)
tacrolimus The hydantoin decreases the effect of tacrolimus (source: Drug Bank)
tacrolimus This combination presents an increased risk of toxicity (source: Drug Bank)
tacrolimus The rifamycin decreases the effect of tacrolimus (source: Drug Bank)
tacrolimus The rifamycin decreases the effect of tacrolimus (source: Drug Bank)
tacrolimus The rifamycin decreases the effect of tacrolimus (source: Drug Bank)
tacrolimus The rifamycin decreases the effect of tacrolimus (source: Drug Bank)
abarelix Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
amikacin Additive renal impairment may occur during concomitant therapy with aminoglycosides such as Amikacin. Use caution during concomitant therapy. (source: Drug Bank)
amiodarone Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
amitriptyline Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
amoxapine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
amphotericin b Additive renal impairment may occur during concomitant therapy with Amphotericin B. Use caution during concomitant therapy. (source: Drug Bank)
amprenavir The protease inhibitor, Amprenavir, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Amprenavir therapy is initiated, discontinued or altered. (source: Drug Bank)
apomorphine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
atazanavir The protease inhibitor, Atazanavir, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Atazanavir therapy is initiated, discontinued or altered. (source: Drug Bank)
bromocriptine Bromocriptine may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Bromocriptine therapy is initiated, discontinued or altered. (source: Drug Bank)
carbamazepine Carbamazepine may decrease the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Carbamazepine therapy is initiated, discontinued or altered. (source: Drug Bank)
caspofungin Caspofungin may decrease the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Caspofungin therapy is initiated, discontinued or altered. (source: Drug Bank)
chloramphenicol Chloramphenicol may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Chloramphenicol therapy is initiated, discontinued or altered. (source: Drug Bank)
chlorpromazine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
cimetidine Cimetidine may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Cimetidine therapy is initiated, discontinued or altered. (source: Drug Bank)
cisapride Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. Cisapride may also increase the concentration of Tacrolimus in the blood. (source: Drug Bank)
cisplatin Additive renal impairment may occur during concomitant therapy with aminoglycosides such as Cisplatin. Use caution during concomitant therapy. (source: Drug Bank)
clarithromycin Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. The macrolide antibiotic, Clarithromycin, may also increase the blood concentration of Tacrolimus. (source: Drug Bank)
clomipramine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
clotrimazole The antifungal, Clotrimazole, may increase serum concentrations of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Clotrimazole therapy is initiated, discontinued or altered. (source: Drug Bank)
conivaptan The strong CYP3A4 inhibitor, Conivaptan, may decrease the metabolism and clearance of Tacrolimus, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Tacrolimus if Conivaptan is initiated, discontinued or dose changed. (source: Drug Bank)
cyclosporine Additive renal impairment may occur during concomitant therapy with Cyclosporine. Combination therapy should be avoided. (source: Drug Bank)
danazol Danazol may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Danazol therapy is initiated, discontinued or altered. (source: Drug Bank)
darunavir The protease inhibitor, Darunavir, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Darunavir therapy is initiated, discontinued or altered. (source: Drug Bank)
dasatinib Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
delavirdine The strong CYP3A4 inhibitor, Delavirdine, may decrease the metabolism and clearance of Tacrolimus, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Tacrolimus if Delavirdine is initiated, discontinued or dose changed. (source: Drug Bank)
desipramine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
diltiazem The calcium channel blocker, Diltiazem, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Diltiazem therapy is initiated, discontinued or altered. (source: Drug Bank)
disopyramide Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
dofetilide Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
dolasetron Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
domperidone Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
doxepin Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
droperidol Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
erythromycin Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. The macrolide antibiotic, Erythromycin, may also increase the blood concentration of Tacrolimus. (source: Drug Bank)
flecainide Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
fluconazole Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. The antifungal, Fluconazole, may also increase serum concentrations of Tacrolimus. (source: Drug Bank)
fluoxetine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
flupenthixol Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
fosamprenavir The protease inhibitor, Fosamprenavir, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Fosamprenavir therapy is initiated, discontinued or altered. (source: Drug Bank)
foscarnet Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
gatifloxacin Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
gentamicin Additive renal impairment may occur during concomitant therapy with aminoglycosides such as Gentamicin. Use caution during concomitant therapy. (source: Drug Bank)
halofantrine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
haloperidol Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
ibutilide Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
imatinib The strong CYP3A4 inhibitor, Imatinib, may decrease the metabolism and clearance of Tacrolimus, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Tacrolimus if Imatinib is initiated, discontinued or dose changed. (source: Drug Bank)
imipramine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
indapamide Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
indinavir The protease inhibitor, Indinavir, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Indinavir therapy is initiated, discontinued or altered. (source: Drug Bank)
isoniazid The strong CYP3A4 inhibitor, Isoniazid, may decrease the metabolism and clearance of Tacrolimus, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Tacrolimus if Isoniazid is initiated, discontinued or dose changed. (source: Drug Bank)
isradipine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
itraconazole The antifungal, Itraconazole, may increase serum concentrations of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Itraconazole therapy is initiated, discontinued or altered. (source: Drug Bank)
ketoconazole The antifungal, Ketoconazole, may increase serum concentrations of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Ketoconzole therapy is initiated, discontinued or altered. (source: Drug Bank)
lapatinib Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
levofloxacin Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
lopinavir The protease inhibitor, Lopinavir, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Lopinavir therapy is initiated, discontinued or altered. (source: Drug Bank)
loxapine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
maprotiline Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
mefloquine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
mesoridazine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
methadone Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
methylprednisolone Methylprednisone may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Methylprednisone therapy is initiated, discontinued or altered. (source: Drug Bank)
metoclopramide Metoclopramide may increase the concentration of Tacrolimus in the blood. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Metoclopramide therapy is initiated, discontinued or altered. (source: Drug Bank)
mibefradil The calcium channel blocker, Mibefradil, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Mibefradil therapy is initiated, discontinued or altered. (source: Drug Bank)
miconazole The strong CYP3A4 inhibitor, Miconazole, may decrease the metabolism and clearance of Tacrolimus, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Tacrolimus if Miconazole is initiated, discontinued or dose changed. (source: Drug Bank)
moxifloxacin Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
natalizumab Tacrolimus may increase the toxic/adverse effects of Natalizumab. Concurrent administration should be avoided due to increased risk of infection. (source: Drug Bank)
nefazodone Nefazodone may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Nefazodone therapy is initiated, discontinued or altered. (source: Drug Bank)
nelfinavir The protease inhibitor, Nelfinavir, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Nelfinavir therapy is initiated, discontinued or altered. (source: Drug Bank)
neomycin Additive renal impairment may occur during concomitant therapy with aminoglycosides such as Neomycin. Use caution during concomitant therapy. (source: Drug Bank)
netilmicin Additive renal impairment may occur during concomitant therapy with aminoglycosides such as Netilmicin. Use caution during concomitant therapy. (source: Drug Bank)
nicardipine The calcium channel blocker, Nicardipine, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Nicardipine therapy is initiated, discontinued or altered. (source: Drug Bank)
nifedipine The calcium channel blocker, Nifedipine, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Nifedipine therapy is initiated, discontinued or altered. (source: Drug Bank)
nilotinib May cause additive QTc-prolonging effects. Concomitant therapy is contraindicated. (source: Drug Bank)
norfloxacin Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
nortriptyline Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
octreotide Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
omeprazole Omeprazole may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Omeprazole therapy is initiated, discontinued or altered. (source: Drug Bank)
paromomycin Additive renal impairment may occur during concomitant therapy with aminoglycosides such as Paromomycin. Use caution during concomitant therapy. (source: Drug Bank)
pentamidine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
perflutren Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
phenobarbital Phenobarbital may decrease the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Phenobarbital therapy is initiated, discontinued or altered. (source: Drug Bank)
phenytoin Phenytoin may decrease the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Phenytoin therapy is initiated, discontinued or altered. (source: Drug Bank)
pimozide Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
posaconazole The strong CYP3A4 inhibitor, Posaconazole, may decrease the metabolism and clearance of Tacrolimus, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Tacrolimus if Posaconazole is initiated, discontinued or dose changed. (source: Drug Bank)
probucol Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
procainamide Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
propafenone Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
protriptyline Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
quetiapine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
quinidine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. Quinidine, a strong CYP3A4 inhibitor, may also increase the serum concentration of Tacrolimus by inhibiting its metabolism and clearance. (source: Drug Bank)
ranolazine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
rifabutin Carbamazepine may decrease the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Carbamazepine therapy is initiated, discontinued or altered. (source: Drug Bank)
rifampin Rifampin may decrease the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Rifampin therapy is initiated, discontinued or altered. (source: Drug Bank)
risperidone Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
ritonavir The protease inhibitor, Ritonavir, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Ritonavir therapy is initiated, discontinued or altered. (source: Drug Bank)
saquinavir The protease inhibitor, Saquinavir, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Saquinavir therapy is initiated, discontinued or altered. (source: Drug Bank)
sirolimus Sirolimus may decrease the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Sirolimus therapy is initiated, discontinued or altered. (source: Drug Bank)
sotalol Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
sparfloxacin Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
streptomycin Additive renal impairment may occur during concomitant therapy with aminoglycosides such as Streptomycin. Use caution during concomitant therapy. (source: Drug Bank)
sunitinib Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
telithromycin Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. Telithromycin, a strong CYP3A4 inhibitor, may also increase the serum concentration of Tacrolimus by inhibiting its metabolism and clearance. (source: Drug Bank)
temsirolimus Temsirolimus may decrease the blood concentration of Tacrolimus. Concomitant therapy may increase the adverse/toxic effects of both agents. Concomitant therapy should be avoided. (source: Drug Bank)
tetrabenazine May cause additive QTc-prolonging effects. Concomitant therapy should be avoided. (source: Drug Bank)
thioridazine May cause additive QTc-prolonging effects. Concomitant therapy is contraindicated. (source: Drug Bank)
thiothixene Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
tipranavir The protease inhibitor, Tipranavir, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Tipranavir therapy is initiated, discontinued or altered. (source: Drug Bank)
tobramycin Additive renal impairment may occur during concomitant therapy with aminoglycosides such as Tobramycin. Use caution during concomitant therapy. (source: Drug Bank)
topotecan The p-glycoprotein inhibitor, Tacrolimus, may increase the bioavailability of Topotecan. Increased Topotecan exposure may result in Topotecan toxicity. This combination should be avoided. (source: Drug Bank)
toremifene Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
trimipramine Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
troleandomycin The macrolide antibiotic, Troleandomycin, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Troleandomycin therapy is initiated, discontinued or altered. (source: Drug Bank)
verapamil The calcium channel blocker, Verapamil, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Verapamil therapy is initiated, discontinued or altered. (source: Drug Bank)
voriconazole Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. The antifungal, Voriconazole, may also increase serum concentrations of Tacrolimus. (source: Drug Bank)
vorinostat Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
ziprasidone May cause additive QTc-prolonging effects. Concomitant therapy is contraindicated. (source: Drug Bank)
zuclopenthixol Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
tacrolimus This antibiotic increases the effect and toxicity of tacrolimus (source: Drug Bank)
tacrolimus Telithromycin may reduce clearance of Tacrolimus. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tacrolimus if Telithromycin is initiated, discontinued or dose changed. (source: Drug Bank)
tacrolimus May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank)
tacrolimus May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank)
tacrolimus Tipranavir may decrease the metabolism and clearance of Tacrolimus. Dose adjustments may be required. Monitor for Tacrolimus efficacy and toxicity during concomitant therapy. (source: Drug Bank)
tacrolimus Increased risk of nephrotoxicity (source: Drug Bank)
tacrolimus The p-glycoprotein inhibitor, Tacrolimus, may increase the bioavailability of oral Topotecan. A clinically significant effect is also expected with IV Topotecan. Concomitant therapy should be avoided. (source: Drug Bank)
tacrolimus Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank)
tacrolimus Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. (source: Drug Bank)
tacrolimus Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of tacrolimus by decreasing its metabolism. Additive QTc prolongation may also occur. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of tacrolimus if voriconazole is initiated, discontinued or dose changed. (source: Drug Bank)
tacrolimus Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank)
tacrolimus Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated. (source: Drug Bank)
tacrolimus Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
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Contraindicated With

Publications related to tacrolimus: 264

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Combined effects of CYP3A5*1, POR*28, and CYP3A4*22 single nucleotide polymorphisms on early concentration-controlled tacrolimus exposure in de-novo renal recipients. Pharmacogenetics and genomics. 2014. Kuypers Dirk R J, et al. PubMed
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The CYP3A4*22 C>T single nucleotide polymorphism is associated with reduced midazolam and tacrolimus clearance in stable renal allograft recipients. The pharmacogenomics journal. 2014. de Jonge H, et al. PubMed
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Effect of CYP3A5*3 on kidney transplant recipients treated with tacrolimus: a systematic review and meta-analysis of observational studies. The pharmacogenomics journal. 2014. Rojas L, et al. PubMed
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Which genetic determinants should be considered for tacrolimus dose optimization in kidney transplantation? A combined analysis of genes affecting the CYP3A locus. Therapeutic drug monitoring. 2014. Bruckmueller Henrike, et al. PubMed
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Influence of TLR4 rs1927907 locus polymorphisms on tacrolimus pharmacokinetics in the early stage after liver transplantation. European journal of clinical pharmacology. 2014. Wang Zhaowen, et al. PubMed
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Pharmacokinetic and CYP3A5 pharmacogenetic differences between once- and twice-daily tacrolimus from the first dosing day to 1 year after renal transplantation. Pharmacogenomics. 2014. Satoh Shigeru, et al. PubMed
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Genetic variance in ABCB1 and CYP3A5 does not contribute toward the development of chronic kidney disease after liver transplantation. Pharmacogenetics and genomics. 2014. Tapirdamaz Ozlem, et al. PubMed
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Impact of cytochrome P450 3A5 polymorphism in graft livers on the frequency of acute cellular rejection in living-donor liver transplantation. Pharmacogenetics and genomics. 2014. Uesugi Miwa, et al. PubMed
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Impact of PPARA and POR polymorphisms on tacrolimus pharmacokinetics and new-onset diabetes in kidney transplant recipients. Pharmacogenetics and genomics. 2014. Kurzawski Mateusz, et al. PubMed
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Calcineurin inhibitors and hypertension: a role for pharmacogenetics?. Pharmacogenomics. 2014. Moes Arthur D, et al. PubMed
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Influence of donor-recipient CYP3A4/5 genotypes, age and fluconazole on tacrolimus pharmacokinetics in pediatric liver transplantation: a population approach. Pharmacogenomics. 2014. Guy-Viterbo Vanessa, et al. PubMed
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Effect of CYP3A5 genotype, steroids, and azoles on tacrolimus in a pediatric renal transplant population. Pediatric nephrology (Berlin, Germany). 2014. Lalan Shwetal, et al. PubMed
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Determination of the most influential sources of variability in tacrolimus trough blood concentrations in adult liver transplant recipients: a bottom-up approach. The AAPS journal. 2014. Gérard Cécile, et al. PubMed
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Clinical implementation of pharmacogenetics in kidney transplantation: calcineurin inhibitors in the starting blocks. British journal of clinical pharmacology. 2014. Elens Laure, et al. PubMed
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The influence of CYP3A, PPARA, and POR genetic variants on the pharmacokinetics of tacrolimus and cyclosporine in renal transplant recipients. European journal of clinical pharmacology. 2014. Lunde Ingrid, et al. PubMed
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CYP3A5 genotypes affect tacrolimus pharmacokinetics and infectious complications in Chinese pediatric liver transplant patients. Pediatric transplantation. 2014. Xue Feng, et al. PubMed
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The impact of genetic polymorphisms on time required to attain the target tacrolimus levels and subsequent pharmacodynamic outcomes in pediatric kidney transplant patients. Saudi journal of kidney diseases and transplantation : an official publication of the Saudi Center for Organ Transplantation, Saudi Arabia. 2014. Shilbayeh Sireen. PubMed
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Influence of cytochrome P450 3A5 polymorphisms on viral infection incidence in kidney transplant patients treated with tacrolimus. Transplantation proceedings. 2014. Hattori Y, et al. PubMed
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Reduced variability of tacrolimus trough level in once-daily tacrolimus-based Taiwanese kidney transplant recipients with high-expressive genotype of cytochrome P450 3A5. Transplantation proceedings. 2014. Wu M-J, et al. PubMed
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Relationship of Cyp3a5 Genotype and Abcb1 Diplotype to Tacrolimus Disposition in Brazilian Kidney Transplant Patients. British journal of clinical pharmacology. 2014. Cusinato D A C, et al. PubMed
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Significant association between CYP3A5 polymorphism and blood concentration of tacrolimus in patients with connective tissue diseases. Journal of human genetics. 2014. Tanaka Kosuke, et al. PubMed
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CYP3A5 and CYP3A4, but not ABCB1 polymorphisms affect tacrolimus dose-adjusted trough concentrations in kidney transplant recipients. Pharmacogenomics. 2014. Kurzawski Mateusz, et al. PubMed
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Personalizing the management of heart failure in congenital heart disease: challenges and opportunities. Pharmacogenomics. 2014. de Denus Simon, et al. PubMed
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Pharmacogenotyping of CYP3A5 in predicting dose-adjusted trough levels of tacrolimus among Malaysian kidney-transplant patients. Canadian journal of physiology and pharmacology. 2014. Hamzah Sharina, et al. PubMed
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Effect of CYP3A4*22, CYP3A5*3, and CYP3A Combined Genotypes on Cyclosporine, Everolimus, and Tacrolimus Pharmacokinetics in Renal Transplantation. CPT: pharmacometrics & systems pharmacology. 2014. Moes D J A R, et al. PubMed
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Association of hemoglobin levels, CYP3A5, and NR1I3 gene polymorphisms with tacrolimus pharmacokinetics in liver transplant patients. Drug metabolism and pharmacokinetics. 2013. Chen Dawei, et al. PubMed
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Utilization of an emr-biorepository to identify the genetic predictors of calcineurin-inhibitor toxicity in heart transplant recipients. Pacific Symposium on Biocomputing. Pacific Symposium on Biocomputing. 2014. Oetjens Matthew, et al. PubMed
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Impact of the CYP3A5, CYP3A4, COMT, IL-10 and POR genetic polymorphisms on tacrolimus metabolism in Chinese renal transplant recipients. PloS one. 2014. Li Chuan-Jiang, et al. PubMed
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Personalized Tacrolimus Dose Requirement by CYP3A5 but Not ABCB1 or ACE Genotyping in Both Recipient and Donor after Pediatric Liver Transplantation. PloS one. 2014. Chen Yi-Kuan, et al. PubMed
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Effects of Combinational CYP3A5 6986A>G Polymorphism in Graft Liver and Native Intestine on the Pharmacokinetics of Tacrolimus in Liver Transplant Patients: A Meta-Analysis. Therapeutic drug monitoring. 2013. Buendia Jefferson A, et al. PubMed
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Population Pharmacokinetic-Pharmacogenetic Model of Tacrolimus in the Early Period after Kidney Transplantation. Basic & clinical pharmacology & toxicology. 2013. Han Nayoung, et al. PubMed
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Clinically actionable genotypes among 10,000 patients with preemptive pharmacogenomic testing. Clinical pharmacology and therapeutics. 2013. Van Driest Sara L, et al. PubMed
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Inclusion of CYP3A5 genotyping in a nonparametric population model improves dosing of tacrolimus early after transplantation. Transplant international : official journal of the European Society for Organ Transplantation. 2013. Asberg Anders, et al. PubMed
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Identification and characterization of a defect CYP3A4 genotype in a kidney transplant patient with severely diminished tacrolimus clearance. Clinical pharmacology and therapeutics. 2013. Werk Anneke Nina, et al. PubMed
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Personalized Tacrolimus Doses Determined by CYP3A5 Genotype for Induction and Maintenance Phases of Kidney Transplantation. Clinical therapeutics. 2013. Vannaprasaht Suda, et al. PubMed
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Effect of CYP3A5*3 Polymorphism on Pharmacokinetic Drug Interaction between Tacrolimus and Amlodipine. Drug metabolism and pharmacokinetics. 2013. Zuo Xiao-Cong, et al. PubMed
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Single-nucleotide polymorphisms in P450 oxidoreductase and peroxisome proliferator-activated receptor-alpha are associated with the development of new-onset diabetes after transplantation in kidney transplant recipients treated with tacrolimus. Pharmacogenetics and genomics. 2013. Elens Laure, et al. PubMed
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A Markov chain model to evaluate the effect of CYP3A5 and ABCB1 polymorphisms on adverse events associated with tacrolimus in pediatric renal transplantation. The AAPS journal. 2013. Sy Sherwin K B, et al. PubMed
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Impact of CYP3A4*22 Allele on Tacrolimus Pharmacokinetics in Early Period After Renal Transplantation: Toward Updated Genotype-Based Dosage Guidelines. Therapeutic drug monitoring. 2013. Elens Laure, et al. PubMed
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Population Pharmacokinetics of Tacrolimus in Adult Kidney Transplant Patients: Impact of CYP3A5 Genotype on Starting Dose. Therapeutic drug monitoring. 2013. Bergmann Troels K, et al. PubMed
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A published pharmacogenetic algorithm was poorly predictive of tacrolimus clearance in an independent cohort of renal transplant recipients. British journal of clinical pharmacology. 2013. Boughton Oliver, et al. PubMed
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Multidrug resistance-associated protein 2 (MRP2/ABCC2) haplotypes significantly affect the pharmacokinetics of tacrolimus in kidney transplant recipients. Clinical pharmacokinetics. 2013. Ogasawara Ken, et al. PubMed
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Pharmaceutical and genetic determinants for interindividual differences of tacrolimus bioavailability in renal transplant recipients. European journal of clinical pharmacology. 2013. Niioka Takenori, et al. PubMed
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Impact of CYP3A5 genotype on tacrolimus versus midazolam clearance in renal transplant recipients: new insights in CYP3A5-mediated drug metabolism. Pharmacogenomics. 2013. de Jonge Hylke, et al. PubMed
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Impact of POR*28 on the Pharmacokinetics of Tacrolimus and Cyclosporine a in Renal Transplant Patients. Therapeutic drug monitoring. 2013. Elens Laure, et al. PubMed
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CYP3A5 Genotype, but Not CYP3A4*1b, CYP3A4*22, or Hematocrit, Predicts Tacrolimus Dose Requirements in Brazilian Renal Transplant Patients. Clinical pharmacology and therapeutics. 2013. Santoro A B, et al. PubMed
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Severe acute nephrotoxicity in a kidney transplant patient despite low tacrolimus levels: a possible interaction between donor and recipient genetic polymorphisms. Journal of clinical pharmacy and therapeutics. 2013. Quaglia M, et al. PubMed
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CYP3A5 genetic polymorphisms affect the pharmacokinetics and short-term remission in patients with ulcerative colitis treated with tacrolimus. Journal of gastroenterology and hepatology. 2013. Hirai Fumihito, et al. PubMed
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PharmGKB summary: cyclosporine and tacrolimus pathways. Pharmacogenetics and genomics. 2013. Barbarino Julia M, et al. PubMed
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Impact of donor and recipient CYP3A5 and ABCB1 genetic polymorphisms on tacrolimus dosage requirements and rejection in Caucasian Spanish liver transplant patients. Journal of clinical pharmacology. 2013. Gómez-Bravo Miguel Angel, et al. PubMed
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Conversion from prograf to advagraf in adolescents with stable liver transplants: Comparative pharmacokinetics and 1-year follow-up. Liver transplantation : official publication of the American Association for the Study of Liver Diseases and the International Liver Transplantation Society. 2013. Carcas-Sansuán Antonio J, et al. PubMed
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Meta-analysis and systematic review of the effect of the donor and recipient CYP3A5 6986A>G genotype on tacrolimus dose requirements in liver transplantation. Pharmacogenetics and genomics. 2013. Rojas Luis E, et al. PubMed
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CYP3A4*22 and CYP3A combined genotypes both correlate with tacrolimus disposition in pediatric heart transplant recipients. Pharmacogenomics. 2013. Gijsen Violette Mgj, et al. PubMed
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Tacrolimus dose requirement in pediatric liver transplantation: influence of CYP3A5 gene polymorphism. Pharmacogenomics. 2013. Durand Philippe, et al. PubMed
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Concentration of tacrolimus and major metabolites in kidney transplant recipients as a function of diabetes mellitus and cytochrome P450 3A gene polymorphism. Xenobiotica; the fate of foreign compounds in biological systems. 2013. Chitnis Shripad D, et al. PubMed
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Population pharmacokinetic and pharmacogenetic analysis of tacrolimus in paediatric liver transplant patients. British journal of clinical pharmacology. 2013. Abdel Jalil Mariam H, et al. PubMed
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The CYP3A4*22 allele affects the predictive value of a pharmacogenetic algorithm predicting tacrolimus predose concentrations. British journal of clinical pharmacology. 2013. Elens Laure, et al. PubMed
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CYP3A4/5 polymorphisms affect the blood level of cyclosporine and tacrolimus in Chinese renal transplant recipients. International journal of clinical pharmacology and therapeutics. 2013. Li Dan-ying, et al. PubMed
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A search for new CYP3A4 variants as determinants of tacrolimus dose requirements in renal-transplanted patients. Pharmacogenetics and genomics. 2013. Tavira Beatriz, et al. PubMed
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CYP3A5 genotype had no impact on intrapatient variability of tacrolimus clearance in renal transplant recipients. Therapeutic drug monitoring. 2013. Spierings N, et al. PubMed
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Challenges in pharmacogenetics. European journal of clinical pharmacology. 2013. Cascorbi Ingolf, et al. PubMed
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Effect of the P450 oxidoreductase 28 polymorphism on the pharmacokinetics of tacrolimus in Chinese healthy male volunteers. European journal of clinical pharmacology. 2013. Zhang Jing-Jing, et al. PubMed
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CYP2C8*3 polymorphism and donor age are associated with allograft dysfunction in kidney transplant recipients treated with calcineurin inhibitors. Journal of clinical pharmacology. 2013. Gervasini Guillermo, et al. PubMed
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Effects of CYP3A4 and CYP3A5 polymorphisms on tacrolimus pharmacokinetics in Chinese adult renal transplant recipients: a population pharmacokinetic analysis. Pharmacogenetics and genomics. 2013. Zuo Xiao-Cong, et al. PubMed
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CYP3A and ABCB1 genetic polymorphisms on the pharmacokinetics and pharmacodynamics of tacrolimus and its metabolites (M-I and M-III). Transplantation. 2013. Yoon Se-Hee, et al. PubMed
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Population pharmacokinetics and pharmacogenetics of once daily prolonged-release formulation of tacrolimus in pediatric and adolescent kidney transplant recipients. European journal of clinical pharmacology. 2013. Zhao Wei, et al. PubMed
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Prediction of the tacrolimus population pharmacokinetic parameters according to CYP3A5 genotype and clinical factors using NONMEM in adult kidney transplant recipients. European journal of clinical pharmacology. 2013. Han Nayoung, et al. PubMed
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Influence of CYP3A4, CYP3A5 and MDR-1 polymorphisms on tacrolimus pharmacokinetics and early renal dysfunction in liver transplant recipients. Gene. 2013. Shi Yunying, et al. PubMed
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Combined approach with therapeutic drug monitoring and pharmacogenomics in renal transplant recipients. Indian journal of nephrology. 2013. Manvizhi S, et al. PubMed
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CYP3A4*22: promising newly identified CYP3A4 variant allele for personalizing pharmacotherapy. Pharmacogenomics. 2013. Elens Laure, et al. PubMed
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Influence of Cytochrome P450 (CYP) 3A4*1G Polymorphism on the Pharmacokinetics of Tacrolimus, Probability of Acute Cellular Rejection, and mRNA Expression Level of CYP3A5 Rather than CYP3A4 in Living-Donor Liver Transplant Patients. Biological & pharmaceutical bulletin. 2013. Uesugi Miwa, et al. PubMed
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Impact of CYP3A5 genetic polymorphism on cross-reactivity in tacrolimus chemiluminescent immunoassay in kidney transplant recipients. Clinica chimica acta; international journal of clinical chemistry. 2012. Hirano Kumi, et al. PubMed
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Novel single nucleotide polymorphisms in interleukin 6 affect tacrolimus metabolism in liver transplant patients. PloS one. 2013. Chen Dawei, et al. PubMed
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The impact of CYP3A5 and MDR1 polymorphisms on tacrolimus dosage requirements and trough concentrations in pediatric renal transplant recipients. Saudi journal of kidney diseases and transplantation : an official publication of the Saudi Center for Organ Transplantation, Saudi Arabia. 2013. Shilbayeh Sireen, et al. PubMed
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Impact of tacrolimus intraindividual variability and CYP3A5 genetic polymorphism on acute rejection in kidney transplantation. Therapeutic drug monitoring. 2012. Ro Han, et al. PubMed
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Genetic differences in Native Americans and tacrolimus dosing after kidney transplantation. Transplantation proceedings. 2013. Chakkera H A, et al. PubMed
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Increased Hospital Stay and Allograft Disfunction in Renal Transplanted Patients with CYP2C19 AA Variant in SNP RS4244285. Drug metabolism and disposition: the biological fate of chemicals. 2012. Boso Virginia, et al. PubMed
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Pharmacogenetics of P450 oxidoreductase: implications in drug metabolism and therapy. Pharmacogenetics and genomics. 2012. Hu Lei, et al. PubMed
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Comparison of pharmacokinetics and pharmacogenetics of once- and twice-daily tacrolimus in the early stage after renal transplantation. Transplantation. 2012. Niioka Takenori, et al. PubMed
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Effect of CYP3A5, CYP3A4, and ABCB1 genotypes as determinants of tacrolimus dose and clinical outcomes after heart transplantation. Transplantation proceedings. 2012. Díaz-Molina B, et al. PubMed
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Effect of CYP3A51/3 polymorphism on blood pressure in renal transplant recipients. Transplantation proceedings. 2012. Torio A, et al. PubMed
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Identification of factors affecting tacrolimus level and 5-year clinical outcome in kidney transplant patients. Basic & clinical pharmacology & toxicology. 2012. Kim In-Wha, et al. PubMed
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Measurement and Compartmental Modeling of the Effect of CYP3A5 Gene Variation on Systemic and Intrarenal Tacrolimus Disposition. Clinical pharmacology and therapeutics. 2012. Zheng S, et al. PubMed
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Combinational effect of intestinal and hepatic CYP3A5 genotypes on tacrolimus pharmacokinetics in recipients of living donor liver transplantation. Transplantation. 2012. Ji Eunhee, et al. PubMed
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In Vivo CYP3A4 Activity, CYP3A5 Genotype, and Hematocrit Predict Tacrolimus Dose Requirements and Clearance in Renal Transplant Patients. Clinical pharmacology and therapeutics. 2012. de Jonge H, et al. PubMed
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Pharmacokinetics of Tacrolimus During Pregnancy. Therapeutic drug monitoring. 2012. Zheng Songmao, et al. PubMed
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The effect of CYP3A5 6986A>G and ABCB1 3435C>T on tacrolimus dose-adjusted trough levels and acute rejection rates in renal transplant patients: a systematic review and meta-analysis. Pharmacogenetics and genomics. 2012. Terrazzino Salvatore, et al. PubMed
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PharmGKB summary: very important pharmacogene information for CYP3A5. Pharmacogenetics and genomics. 2012. Lamba Jatinder, et al. PubMed
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Validation of tacrolimus equation to predict troughs using genetic and clinical factors. Pharmacogenomics. 2012. Passey Chaitali, et al. PubMed
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The Dual Role of Pharmacogenetics in HIV Treatment: Mutations and Polymorphisms Regulating Antiretroviral Drug Resistance and Disposition. Pharmacological reviews. 2012. Michaud Veronique, et al. PubMed
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Frequencies of CYP3A5*1/*3 variants in a Moroccan population and effect on tacrolimus daily dose requirements in renal transplant patients. Genetic testing and molecular biomarkers. 2012. Elmachad Mustapha, et al. PubMed
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CYP3A5 polymorphism in Mexican renal transplant recipients and its association with tacrolimus dosing. Archives of medical research. 2012. García-Roca Pilar, et al. PubMed
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Clinical and genetic factors affecting tacrolimus trough levels and drug-related outcomes in Korean kidney transplant recipients. European journal of clinical pharmacology. 2012. Kim In-Wha, et al. PubMed
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The interactions of age, sex, body mass index, genetics, and steroid weight-based doses on tacrolimus dosing requirement after adult kidney transplantation. European journal of clinical pharmacology. 2012. Stratta P, et al. PubMed
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Unusual high dose of tacrolimus in liver transplant patient, a case report. International journal of clinical pharmacy. 2012. Provenzani Alessio, et al. PubMed
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Impact of genetic polymorphisms on tacrolimus pharmacokinetics and the clinical outcome of renal transplantation. Transplant international : official journal of the European Society for Organ Transplantation. 2012. Gervasini Guillermo, et al. PubMed
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Population pharmacokinetic modelling and design of a Bayesian estimator for therapeutic drug monitoring of tacrolimus in lung transplantation. Clinical pharmacokinetics. 2012. Monchaud Caroline, et al. PubMed
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Influence of NAT2 polymorphisms on sulfamethoxazole pharmacokinetics in renal transplant recipients. Antimicrobial agents and chemotherapy. 2012. Kagaya Hideaki, et al. PubMed
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Association between tacrolimus concentration and genetic polymorphisms of CYP3A5 and ABCB1 during the early stage after liver transplant in an Iranian population. Experimental and clinical transplantation : official journal of the Middle East Society for Organ Transplantation. 2012. Rahsaz Marjan, et al. PubMed
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The use of a DNA biobank linked to electronic medical records to characterize pharmacogenomic predictors of tacrolimus dose requirement in kidney transplant recipients. Pharmacogenetics and genomics. 2012. Birdwell Kelly A, et al. PubMed
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Impact of cytochrome P450 3A and ATP-binding cassette subfamily B member 1 polymorphisms on tacrolimus dose-adjusted trough concentrations among Korean renal transplant recipients. Transplantation proceedings. 2012. Cho J-H, et al. PubMed
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Dosing equation for tacrolimus using genetic variants and clinical factors. British journal of clinical pharmacology. 2011. Passey Chaitali, et al. PubMed
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The interactions of age, genetics, and disease severity on tacrolimus dosing requirements after pediatric kidney and liver transplantation. European journal of clinical pharmacology. 2011. de Wildt Saskia N, et al. PubMed
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Influence of CYP3A5 and ABCB1 gene polymorphisms and other factors on tacrolimus dosing in Caucasian liver and kidney transplant patients. International journal of molecular medicine. 2011. Provenzani Alessio, et al. PubMed
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Age and CYP3A5 genotype affect tacrolimus dosing requirements after transplant in pediatric heart recipients. The Journal of heart and lung transplantation : the official publication of the International Society for Heart Transplantation. 2011. Gijsen Violette, et al. PubMed
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A new functional CYP3A4 intron 6 polymorphism significantly affects tacrolimus pharmacokinetics in kidney transplant recipients. Clinical chemistry. 2011. Elens Laure, et al. PubMed
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Lower tacrolimus daily dose requirements and acute rejection rates in the CYP3A5 nonexpressers than expressers. Pharmacogenetics and genomics. 2011. Tang Hui-Lin, et al. PubMed
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Population Pharmacokinetics and Pharmacogenetics of Tacrolimus in Healthy Chinese Volunteers. Pharmacology. 2011. Xue Ling, et al. PubMed
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Association of ABCB1, CYP3A4*18B and CYP3A5*3 genotypes with the pharmacokinetics of tacrolimus in healthy Chinese subjects: a population pharmacokinetic analysis. Journal of clinical pharmacy and therapeutics. 2011. Shi X-J, et al. PubMed
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In vivo CYP3A activity is significantly lower in cyclosporine-treated as compared with tacrolimus-treated renal allograft recipients. Clinical pharmacology and therapeutics. 2011. de Jonge H, et al. PubMed
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CYP3A5 and ABCB1 polymorphisms in donor and recipient: impact on Tacrolimus dose requirements and clinical outcome after renal transplantation. Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association. 2011. Glowacki François, et al. PubMed
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Effect of a new functional CYP3A4 polymorphism on calcineurin inhibitors dose requirements and trough blood levels in stable renal transplant patients. Pharmacogenomics. 2011. Elens Laure, et al. PubMed
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Pharmacogenetics of calcineurin inhibitors in Brazilian renal transplant patients. Pharmacogenomics. 2011. Santoro Ana, et al. PubMed
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The P450 oxidoreductase *28 SNP is associated with low initial tacrolimus exposure and increased dose requirements in CYP3A5-expressing renal recipients. Pharmacogenomics. 2011. de Jonge Hylke, et al. PubMed
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Cytochrome P450 genetic polymorphisms influence the serum concentration of calcineurin inhibitors in allogeneic hematopoietic SCT recipients. Bone marrow transplantation. 2011. Onizuka M, et al. PubMed
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Impact of interleukin-10 gene polymorphisms on tacrolimus dosing requirements in Chinese liver transplant patients during the early posttransplantation period. European journal of clinical pharmacology. 2011. Zhang Xiaoqing, et al. PubMed
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Tacrolimus dosing in Chinese renal transplant recipients: a population-based pharmacogenetics study. European journal of clinical pharmacology. 2011. Li Liang, et al. PubMed
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Influence of CYP3A5 polymorphism on tacrolimus maintenance doses and serum levels after renal transplantation: age dependency and pharmacological interaction with steroids. Pediatric transplantation. 2011. Ferraris Jorge R, et al. PubMed
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Influence of cytochrome P450 3A5 (CYP3A5) genetic polymorphism on the pharmacokinetics of the prolonged-release, once-daily formulation of tacrolimus in stable renal transplant recipients. Clinical pharmacokinetics. 2011. Glowacki François, et al. PubMed
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Impact of the CYP3A4*1G polymorphism and its combination with CYP3A5 genotypes on tacrolimus pharmacokinetics in renal transplant patients. Pharmacogenomics. 2011. Miura Masatomo, et al. PubMed
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Pharmacogenetics and individualized therapy in children: immunosuppressants, antidepressants, anticancer and anti-inflammatory drugs. Pharmacogenomics. 2011. Elie Valery, et al. PubMed
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A low-risk ZnT-8 allele (W325) for post-transplantation diabetes mellitus is protective against cyclosporin A-induced impairment of insulin secretion. The pharmacogenomics journal. 2011. Kim I, et al. PubMed
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CYP3A5 genotype is not related to the intrapatient variability of tacrolimus clearance. Therapeutic drug monitoring. 2011. Pashaee Nilufar, et al. PubMed
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Pharmacogenetics of tacrolimus after renal transplantation: analysis of polymorphisms in genes encoding 16 drug metabolizing enzymes. Clinical chemistry and laboratory medicine : CCLM / FESCC. 2011. Tavira Beatriz, et al. PubMed
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Expression of CYP3A5 and P-glycoprotein in renal allografts with histological signs of calcineurin inhibitor nephrotoxicity. Transplantation. 2011. Metalidis Christoph, et al. PubMed
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Pharmacogenetic determinants for interindividual difference of tacrolimus pharmacokinetics 1 year after renal transplantation. Journal of clinical pharmacy and therapeutics. 2011. Miura M, et al. PubMed
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Differential impact of the CYP3A5*1 and CYP3A5*3 alleles on pre-dose concentrations of two tacrolimus formulations. Pharmacogenetics and genomics. 2011. Wehland Markus, et al. PubMed
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ABCB1 Single-Nucleotide Polymorphisms Determine Tacrolimus Response in Patients With Ulcerative Colitis. Clinical pharmacology and therapeutics. 2011. Herrlinger K R, et al. PubMed
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Drug Interactions Between the Immunosuppressant Tacrolimus and the Cholesterol Absorption Inhibitor Ezetimibe in Healthy Volunteers. Clinical pharmacology and therapeutics. 2011. Oswald S, et al. PubMed
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Pharmacogenomics of the RNA world: structural RNA polymorphisms in drug therapy. Clinical pharmacology and therapeutics. 2011. Sadee W, et al. PubMed
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KCNQ1 gene variants and risk of new-onset diabetes in tacrolimus-treated renal-transplanted patients. Clinical transplantation. 2011. Tavira Beatriz, et al. PubMed
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Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein). Pharmacogenetics and genomics. 2011. Hodges Laura M, et al. PubMed
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Seasonal variation in blood drug concentrations and a potential relationship to vitamin D. Drug metabolism and disposition: the biological fate of chemicals. 2011. Lindh Jonatan D, et al. PubMed
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Novel polymorphisms associated with tacrolimus trough concentrations: results from a multicenter kidney transplant consortium. Transplantation. 2011. Jacobson Pamala A, et al. PubMed
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Engraftment syndrome, but not acute GVHD, younger age, CYP3A5 or MDR1 polymorphisms, increases tacrolimus clearance in pediatric hematopoietic SCT. Bone marrow transplantation. 2011. Yanagisawa R, et al. PubMed
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Practical recommendations for pharmacogenomics-based prescription: 2010 ESF-UB Conference on Pharmacogenetics and Pharmacogenomics. Pharmacogenomics. 2011. Becquemont Laurent, et al. PubMed
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Impact of CYP3A5 genotype of recipients as well as donors on the tacrolimus pharmacokinetics and infectious complications after living-donor liver transplantation for Japanese adult recipients. Annals of transplantation : quarterly of the Polish Transplantation Society. 2011. Muraki Yuichi, et al. PubMed
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Polymorphisms in CYP3A5*3 and MDR1, and haplotype modulate response to plasma levels of tacrolimus in Chinese renal transplant patients. Annals of transplantation : quarterly of the Polish Transplantation Society. 2011. Wu Ping, et al. PubMed
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Association between CYP3A5 polymorphisms and blood pressure in kidney transplant recipients receiving calcineurin inhibitors. Clinical and experimental hypertension (New York, N.Y. : 1993). 2011. Ferraresso Mariano, et al. PubMed
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The role of CYP3A5 genotypes in dose requirements of tacrolimus and everolimus after heart transplantation. Clinical transplantation. 2011. Kniepeiss Daniela, et al. PubMed
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Successful tacrolimus treatment following renal transplant in a HIV-infected patient with raltegravir previously treated with a protease inhibitor based regimen. Drug metabolism and drug interactions. 2011. Cousins Darren, et al. PubMed
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CYP3A5 *1 allele: impacts on early acute rejection and graft function in tacrolimus-based renal transplant recipients. Transplantation. 2010. Min Sang-Il, et al. PubMed
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Pharmacogenetic study of ABCB1 and CYP3A5 genes during the first year following heart transplantation regarding tacrolimus or cyclosporine levels. Transplantation proceedings. 2011. Jordán de Luna C, et al. PubMed
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Pharmacogenetic vs. concentration-controlled optimization of tacrolimus dosing in renal allograft recipients. Clinical pharmacology and therapeutics. 2010. Kuypers D R J. PubMed
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Influence of CYP3A5 and ABCB1 gene polymorphisms on calcineurin inhibitor-related neurotoxicity after hematopoietic stem cell transplantation. Clinical transplantation. 2010. Yanagimachi Masakatsu, et al. PubMed
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Influence of CYP3A5 and MDR1(ABCB1) polymorphisms on the pharmacokinetics of tacrolimus in Chinese renal transplant recipients. Transplantation proceedings. 2010. Rong G, et al. PubMed
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Value of CYP3A5 genotyping on determining initial dosages of tacrolimus for Chinese renal transplant recipients. Transplantation proceedings. 2010. Zhang J, et al. PubMed
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Population pharmacokinetics and Bayesian estimation of tacrolimus exposure in renal transplant recipients on a new once-daily formulation. Clinical pharmacokinetics. 2010. Benkali Khaled, et al. PubMed
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Deciphering calcineurin inhibitor nephrotoxicity: a pharmacological approach. Pharmacogenomics. 2010. Pallet Nicolas, et al. PubMed
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Using genetic and clinical factors to predict tacrolimus dose in renal transplant recipients. Pharmacogenomics. 2010. Wang Ping, et al. PubMed
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Genetic polymorphisms and individualized tacrolimus dosing. Transplantation proceedings. 2010. López-Montenegro Soria M A, et al. PubMed
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Correlation of IMPDH1 gene polymorphisms with subclinical acute rejection and mycophenolic acid exposure parameters on day 28 after renal transplantation. Basic & clinical pharmacology & toxicology. 2010. Kagaya Hideaki, et al. PubMed
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Tacrolimus dose requirements and CYP3A5 genotype and the development of calcineurin inhibitor-associated nephrotoxicity in renal allograft recipients. Therapeutic drug monitoring. 2010. Kuypers Dirk R J, et al. PubMed
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Prediction of adverse drug reactions using decision tree modeling. Clinical pharmacology and therapeutics. 2010. Hammann F, et al. PubMed
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Effect of gene polymorphisms on the levels of calcineurin inhibitors in Indian renal transplant recipients. Indian journal of nephrology. 2010. Ashavaid T, et al. PubMed
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Risk of diarrhoea in a long-term cohort of renal transplant patients given mycophenolate mofetil: the significant role of the UGT1A8 2 variant allele. British journal of clinical pharmacology. 2010. Woillard Jean-Baptiste, et al. PubMed
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Dosing tacrolimus based on CYP3A5 genotype: will it improve clinical outcome?. Clinical pharmacology and therapeutics. 2010. van Gelder T, et al. PubMed
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Optimization of initial tacrolimus dose using pharmacogenetic testing. Clinical pharmacology and therapeutics. 2010. Thervet E, et al. PubMed
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Effects of diltiazem on pharmacokinetics of tacrolimus in relation to CYP3A5 genotype status in renal recipients: from retrospective to prospective. The pharmacogenomics journal. 2010. Li J-L, et al. PubMed
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Use of pharmacogenetics to optimize immunosuppressive therapy. Therapeutic drug monitoring. 2010. Macphee Iain A M. PubMed
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Tacrolimus nephrotoxicity: beware of the association of diarrhea, drug interaction and pharmacogenetics. Pediatric nephrology (Berlin, Germany). 2010. Leroy Sandrine, et al. PubMed
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CYP3A5 and ABCB1 polymorphisms influence tacrolimus concentrations in peripheral blood mononuclear cells after renal transplantation. Pharmacogenomics. 2010. Capron Arnaud, et al. PubMed
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Effect of CYP3A and ABCB1 single nucleotide polymorphisms on the pharmacokinetics and pharmacodynamics of calcineurin inhibitors: Part II. Clinical pharmacokinetics. 2010. Staatz Christine E, et al. PubMed
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An integrative approach for identifying a metabolic phenotype predictive of individualized pharmacokinetics of tacrolimus. Clinical pharmacology and therapeutics. 2010. Phapale P B, et al. PubMed
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Association of calpain-10 gene polymorphism and posttransplant diabetes mellitus in kidney transplant patients medicated with tacrolimus. The pharmacogenomics journal. 2010. Kurzawski Mateusz, et al. PubMed
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Effect of CYP3A and ABCB1 single nucleotide polymorphisms on the pharmacokinetics and pharmacodynamics of calcineurin inhibitors: Part I. Clinical pharmacokinetics. 2010. Staatz Christine E, et al. PubMed
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The role of organic anion-transporting polypeptides and their common genetic variants in mycophenolic acid pharmacokinetics. Clinical pharmacology and therapeutics. 2010. Picard N, et al. PubMed
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Population pharmacokinetics and pharmacogenetics of tacrolimus in de novo pediatric kidney transplant recipients. Clinical pharmacology and therapeutics. 2009. Zhao W, et al. PubMed
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Factors affecting the long-term response to tacrolimus in renal transplant patients: pharmacokinetic and pharmacogenetic approach. International journal of medical sciences. 2010. Katsakiori Paraskevi F, et al. PubMed
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Frequencies and roles of CYP3A5, CYP3A4 and ABCB1 single nucleotide polymorphisms in Italian teenagers after kidney transplantation. Pharmacological reports : PR. 2010. Turolo Stefano, et al. PubMed
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Pharmacogenetics of immunosuppressant polymorphism of CYP3A5 in renal transplant recipients. Transplantation proceedings. 2010. Larriba J, et al. PubMed
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Donor age and renal P-glycoprotein expression associate with chronic histological damage in renal allografts. Journal of the American Society of Nephrology : JASN. 2009. Naesens Maarten, et al. PubMed
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TCF7L2 polymorphism associates with new-onset diabetes after transplantation. Journal of the American Society of Nephrology : JASN. 2009. Ghisdal Lidia, et al. PubMed
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Increased mycophenolic acid exposure in stable kidney transplant recipients on tacrolimus as compared with those on sirolimus: implications for pharmacokinetics. Clinical pharmacology and therapeutics. 2009. Braun F, et al. PubMed
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UGT1A9 -275T>A/-2152C>T polymorphisms correlate with low MPA exposure and acute rejection in MMF/tacrolimus-treated kidney transplant patients. Clinical pharmacology and therapeutics. 2009. van Schaik R H N, et al. PubMed
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Impact of CYP3A5 and CYP3A4 gene polymorphisms on dose requirement of calcineurin inhibitors, cyclosporine and tacrolimus, in renal allograft recipients of North India. Naunyn-Schmiedeberg's archives of pharmacology. 2009. Singh Ranjana, et al. PubMed
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Pharmacogenetics of calcineurin inhibitors in renal transplantation. Transplantation. 2009. Coto Eliecer, et al. PubMed
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Histone deacetylase inhibitors induce a very broad, pleiotropic anticancer drug resistance phenotype in acute myeloid leukemia cells by modulation of multiple ABC transporter genes. Clinical cancer research : an official journal of the American Association for Cancer Research. 2009. Hauswald Stefanie, et al. PubMed
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Effect of CYP3A5 genotype on renal allograft recipients treated with tacrolimus. Transplantation proceedings. 2009. Chen J S, et al. PubMed
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CYP3A5 *1 allele associated with tacrolimus trough concentrations but not subclinical acute rejection or chronic allograft nephropathy in Japanese renal transplant recipients. European journal of clinical pharmacology. 2009. Satoh Shigeru, et al. PubMed
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Genetic determinants of response to clopidogrel and cardiovascular events. The New England journal of medicine. 2009. Simon Tabassome, et al. PubMed
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Explaining variability in tacrolimus pharmacokinetics to optimize early exposure in adult kidney transplant recipients. Therapeutic drug monitoring. 2009. Press Rogier R, et al. PubMed
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Tacrolimus concentrations in relation to CYP3A and ABCB1 polymorphisms among solid organ transplant recipients in Korea. Transplantation. 2009. Jun Kyung Ran, et al. PubMed
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Redox regulation of multidrug resistance in cancer chemotherapy: molecular mechanisms and therapeutic opportunities. Antioxidants & redox signaling. 2009. Kuo Macus Tien. PubMed
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Evaluation of the genetic background of standard-immunosuppressant-related toxicity in a cohort of 200 paediatric renal allograft recipients--a retrospective study. Annals of transplantation : quarterly of the Polish Transplantation Society. 2009. Grenda Ryszard, et al. PubMed
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The effect of CYP3A5 and ABCB1 single nucleotide polymorphisms on tacrolimus dose requirements in Caucasian liver transplant patients. Annals of transplantation : quarterly of the Polish Transplantation Society. 2009. Provenzani Alessio, et al. PubMed
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Influence of CYP3A5 genetic polymorphism on tacrolimus daily dose requirements and acute rejection in renal graft recipients. Basic & clinical pharmacology & toxicology. 2008. Quteineh Lina, et al. PubMed
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Several major antiepileptic drugs are substrates for human P-glycoprotein. Neuropharmacology. 2008. Luna-Tortós Carlos, et al. PubMed
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Role of cytochrome P450 2C8 and 2J2 genotypes in calcineurin inhibitor-induced chronic kidney disease. Pharmacogenetics and genomics. 2008. Smith Helen E, et al. PubMed
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Effects of CYP3A5 and MDR1 single nucleotide polymorphisms on drug interactions between tacrolimus and fluconazole in renal allograft recipients. Pharmacogenetics and genomics. 2008. Kuypers Dirk R, et al. PubMed
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Genetic variation in drug transporters in ethnic populations. Clinical pharmacology and therapeutics. 2008. Cropp C D, et al. PubMed
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Lack of tacrolimus circadian pharmacokinetics and CYP3A5 pharmacogenetics in the early and maintenance stages in Japanese renal transplant recipients. British journal of clinical pharmacology. 2008. Satoh Shigeru, et al. PubMed
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Pharmacogenomic associations in ABCB1 and CYP3A5 with acute kidney injury and chronic kidney disease after myeloablative hematopoietic cell transplantation. The pharmacogenomics journal. 2008. Woodahl E L, et al. PubMed
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Impact of CYP3A5 genetic polymorphism on pharmacokinetics of tacrolimus in healthy Japanese subjects. British journal of clinical pharmacology. 2008. Suzuki Yoshiharu, et al. PubMed
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No association between single nucleotide polymorphisms and the development of nephrotoxicity after orthotopic heart transplantation. The Journal of heart and lung transplantation : the official publication of the International Society for Heart Transplantation. 2008. Klauke Bärbel, et al. PubMed
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Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition. Xenobiotica; the fate of foreign compounds in biological systems. 2008. Zhou S-F. PubMed
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Significant impact of gene polymorphisms on tacrolimus but not cyclosporine dosing in Asian renal transplant recipients. Transplantation proceedings. 2008. Loh P T, et al. PubMed
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The effect of CYP3A5 polymorphisms on the pharmacokinetics of tacrolimus in adolescent kidney transplant recipients. Medical science monitor : international medical journal of experimental and clinical research. 2008. Tirelli Silvia, et al. PubMed
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Impact of MDR1 and CYP3A5 on the oral clearance of tacrolimus and tacrolimus-related renal dysfunction in adult living-donor liver transplant patients. Pharmacogenetics and genomics. 2008. Fukudo Masahide, et al. PubMed
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CYP3A5 genotype is not associated with a higher risk of acute rejection in tacrolimus-treated renal transplant recipients. Pharmacogenetics and genomics. 2008. Hesselink Dennis A, et al. PubMed
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Polymorphisms in the drug transporter gene ABCB1 predict antidepressant treatment response in depression. Neuron. 2008. Uhr Manfred, et al. PubMed
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Citalopram enantiomers in plasma and cerebrospinal fluid of ABCB1 genotyped depressive patients and clinical response: a pilot study. Pharmacological research : the official journal of the Italian Pharmacological Society. 2008. Nikisch Georg, et al. PubMed
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CYP3A5 and CYP3A4 but not MDR1 single-nucleotide polymorphisms determine long-term tacrolimus disposition and drug-related nephrotoxicity in renal recipients. Clinical pharmacology and therapeutics. 2007. Kuypers D R J, et al. PubMed
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Population pharmacokinetics of tacrolimus and CYP3A5, MDR1 and IL-10 polymorphisms in adult liver transplant patients. Journal of clinical pharmacy and therapeutics. 2007. Li D, et al. PubMed
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1199G>A and 2677G>T/A polymorphisms of ABCB1 independently affect tacrolimus concentration in hepatic tissue after liver transplantation. Pharmacogenetics and genomics. 2007. Elens Laure, et al. PubMed
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Influence of the CYP3A5 and MDR1 genetic polymorphisms on the pharmacokinetics of tacrolimus in healthy Korean subjects. British journal of clinical pharmacology. 2007. Choi Ji H, et al. PubMed
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Polymorphisms of tumor necrosis factor-alpha, interleukin-10, cytochrome P450 3A5 and ABCB1 in Chinese liver transplant patients treated with immunosuppressant tacrolimus. Clinica chimica acta; international journal of clinical chemistry. 2007. Li Dan, et al. PubMed
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Tacrolimus pharmacokinetics and pharmacogenetics: influence of adenosine triphosphate-binding cassette B1 (ABCB1) and cytochrome (CYP) 3A polymorphisms. Fundamental & clinical pharmacology. 2007. Op den Buijsch Robert A M, et al. PubMed
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Cytochrome P450 3A polymorphisms and immunosuppressive drugs: an update. Pharmacogenomics. 2007. Anglicheau Dany, et al. PubMed
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Influence of the CYP3A5 genotype on tacrolimus pharmacokinetics and pharmacodynamics in young kidney transplant recipients. Pediatric transplantation. 2007. Ferraresso Mariano, et al. PubMed
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CYP3A5 genotype markedly influences the pharmacokinetics of tacrolimus and sirolimus in kidney transplant recipients. Clinical pharmacology and therapeutics. 2007. Renders L, et al. PubMed
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Cobalamin potentiates vinblastine cytotoxicity through downregulation of mdr-1 gene expression in HepG2 cells. Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology. 2007. Marguerite Véronique, et al. PubMed
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Influence of ABCB1 C3435T polymorphism on the pharmacokinetics of lansoprazole and gastroesophageal symptoms in Japanese renal transplant recipients classified as CYP2C19 extensive metabolizers and treated with tacrolimus. International journal of clinical pharmacology and therapeutics. 2006. Miura M, et al. PubMed
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Mechanism of inhibition of P-glycoprotein mediated efflux by vitamin E TPGS: influence on ATPase activity and membrane fluidity. Molecular pharmaceutics. 2007. Collnot Eva-Maria, et al. PubMed
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CYP3A5 and ABCB1 polymorphisms and tacrolimus pharmacokinetics in renal transplant candidates: guidelines from an experimental study. American journal of transplantation : official journal of the American Society of Transplantation and the American Society of Transplant Surgeons. 2006. Haufroid V, et al. PubMed
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Population pharmacokinetic and pharmacogenomic analysis of tacrolimus in pediatric living-donor liver transplant recipients. Clinical pharmacology and therapeutics. 2006. Fukudo Masahide, et al. PubMed
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Cyclosporin A, tacrolimus and sirolimus are potent inhibitors of the human breast cancer resistance protein (ABCG2) and reverse resistance to mitoxantrone and topotecan. Cancer chemotherapy and pharmacology. 2006. Gupta Anshul, et al. PubMed
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Cyp3A4, Cyp3A5, and MDR-1 genetic influences on tacrolimus pharmacokinetics in renal transplant recipients. Pharmacogenetics and genomics. 2006. Roy Jean Nicholas, et al. PubMed
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Drug-drug interaction between pitavastatin and various drugs via OATP1B1. Drug metabolism and disposition: the biological fate of chemicals. 2006. Hirano Masaru, et al. PubMed
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Influence of different allelic variants of the CYP3A and ABCB1 genes on the tacrolimus pharmacokinetic profile of Chinese renal transplant recipients. Pharmacogenomics. 2006. Cheung Chi Yuen, et al. PubMed
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Gefitinib modulates the function of multiple ATP-binding cassette transporters in vivo. Cancer research. 2006. Leggas Markos, et al. PubMed
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Impact of P-glycoprotein on clopidogrel absorption. Clinical pharmacology and therapeutics. 2006. Taubert Dirk, et al. PubMed
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Effect of CYP3A5 polymorphism on tacrolimus metabolic clearance in vitro. Drug metabolism and disposition: the biological fate of chemicals. 2006. Dai Yang, et al. PubMed
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Tacrolimus dose requirement in relation to donor and recipient ABCB1 and CYP3A5 gene polymorphisms in Chinese liver transplant patients. Liver transplantation : official publication of the American Association for the Study of Liver Diseases and the International Liver Transplantation Society. 2006. Wei-lin Wang, et al. PubMed
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Effect of intestinal CYP3A5 on postoperative tacrolimus trough levels in living-donor liver transplant recipients. Pharmacogenetics and genomics. 2006. Uesugi Miwa, et al. PubMed
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Intestinal MDR1/ABCB1 level at surgery as a risk factor of acute cellular rejection in living-donor liver transplant patients. Clinical pharmacology and therapeutics. 2006. Masuda Satohiro, et al. PubMed
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Single nucleotide polymorphisms in human P-glycoprotein: its impact on drug delivery and disposition. Expert opinion on drug delivery. 2006. Dey Surajit. PubMed
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Influence of CYP3A5 gene polymorphisms of donor rather than recipient to tacrolimus individual dose requirement in liver transplantation. Transplantation. 2006. Yu Songfeng, et al. PubMed
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The influence of genetic polymorphisms of cytochrome P450 3A5 and ABCB1 on starting dose- and weight-standardized tacrolimus trough concentrations after kidney transplantation in relation to renal function. Clinical chemistry and laboratory medicine : CCLM / FESCC. 2006. Mourad Michel, et al. PubMed
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Influence of CYP3A5 and MDR1 polymorphisms on tacrolimus concentration in the early stage after renal transplantation. Clinical transplantation. 2005. Zhang Xin, et al. PubMed
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Sirolimus and tacrolimus trough concentrations and dose requirements after kidney transplantation in relation to CYP3A5 and MDR1 polymorphisms and steroids. Transplantation. 2005. Mourad Michel, et al. PubMed
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Impact of CYP3A5 and MDR1(ABCB1) C3435T polymorphisms on the pharmacokinetics of tacrolimus in renal transplant recipients. Transplantation proceedings. 2005. Tada H, et al. PubMed
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Sequential analysis of tacrolimus dosing in adult lung transplant patients with ABCB1 haplotypes. Journal of clinical pharmacology. 2005. Zheng Hongxia, et al. PubMed
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Tacrolimus pharmacogenetics: the CYP3A5*1 allele predicts low dose-normalized tacrolimus blood concentrations in whites and South Asians. Transplantation. 2005. Macphee Iain A M, et al. PubMed
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Genetic polymorphisms of CYP3A5 genes and concentration of the cyclosporine and tacrolimus. Transplantation proceedings. 2005. Zhao Y, et al. PubMed
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MDR1 haplotypes derived from exons 21 and 26 do not affect the steady-state pharmacokinetics of tacrolimus in renal transplant patients. British journal of clinical pharmacology. 2004. Mai Ingrid, et al. PubMed
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Influence of CYP3A5 and MDR1 (ABCB1) polymorphisms on the pharmacokinetics of tacrolimus in renal transplant recipients. Transplantation. 2004. Tsuchiya Norihiko, et al. PubMed
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Tacrolimus therapy in rheumatoid arthritis. Rheumatology (Oxford, England). 2004. McCarey D W, et al. PubMed
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CYP3A5*1-carrying graft liver reduces the concentration/oral dose ratio of tacrolimus in recipients of living-donor liver transplantation. Pharmacogenetics. 2004. Goto Maki, et al. PubMed
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The influence of pharmacogenetics on the time to achieve target tacrolimus concentrations after kidney transplantation. American journal of transplantation : official journal of the American Society of Transplantation and the American Society of Transplant Surgeons. 2004. MacPhee Iain A M, et al. PubMed
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Influence of lipid lowering fibrates on P-glycoprotein activity in vitro. Biochemical pharmacology. 2004. Ehrhardt Manuela, et al. PubMed
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Interactions of human P-glycoprotein with simvastatin, simvastatin acid, and atorvastatin. Pharmaceutical research. 2004. Hochman Jerome H, et al. PubMed
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The effect of CYP3A5 and MDR1 (ABCB1) polymorphisms on cyclosporine and tacrolimus dose requirements and trough blood levels in stable renal transplant patients. Pharmacogenetics. 2004. Haufroid Vincent, et al. PubMed
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Pharmacology of calcineurin antagonists. Transplantation proceedings. 2004. Kapturczak M H, et al. PubMed
Tacrolimus dosing in adult lung transplant patients is related to cytochrome P4503A5 gene polymorphism. Journal of clinical pharmacology. 2004. Zheng HongXia, et al. PubMed
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Polymorphisms in human MDR1 (P-glycoprotein): recent advances and clinical relevance. Clinical pharmacology and therapeutics. 2004. Marzolini Catia, et al. PubMed
ABCB1 C3435T and G2677T/A polymorphism decreased the risk for steroid-induced osteonecrosis of the femoral head after kidney transplantation. Pharmacogenetics. 2003. Asano Takeshi, et al. PubMed
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Impact of cytochrome p450 3A5 genetic polymorphism on tacrolimus doses and concentration-to-dose ratio in renal transplant recipients. Transplantation. 2003. Thervet Eric, et al. PubMed
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Genetic polymorphisms of the CYP3A4, CYP3A5, and MDR-1 genes and pharmacokinetics of the calcineurin inhibitors cyclosporine and tacrolimus. Clinical pharmacology and therapeutics. 2003. Hesselink Dennis A, et al. PubMed
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Tacrolimus dosing in pediatric heart transplant patients is related to CYP3A5 and MDR1 gene polymorphisms. American journal of transplantation : official journal of the American Society of Transplantation and the American Society of Transplant Surgeons. 2003. Zheng HongXia, et al. PubMed
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Genetic polymorphisms of the human MDR1 drug transporter. Annual review of pharmacology and toxicology. 2003. Schwab Matthias, et al. PubMed
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Atopic dermatitis management with tacrolimus ointment (Protopic). The Journal of dermatological treatment. 2003. Kapp A, et al. PubMed
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Tacrolimus pharmacogenetics: polymorphisms associated with expression of cytochrome p4503A5 and P-glycoprotein correlate with dose requirement. Transplantation. 2002. Macphee Iain A M, et al. PubMed
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The MDR1 polymorphisms at exons 21 and 26 predict steroid weaning in pediatric heart transplant patients. Human immunology. 2002. Zheng HongXia, et al. PubMed
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C3435T polymorphism in the MDR1 gene affects the enterocyte expression level of CYP3A4 rather than Pgp in recipients of living-donor liver transplantation. Pharmacogenetics. 2002. Goto Maki, et al. PubMed
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Neurotoxicity induced by tacrolimus after liver transplantation: relation to genetic polymorphisms of the ABCB1 (MDR1) gene. Transplantation. 2002. Yamauchi Atsushi, et al. PubMed
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Interaction of omeprazole, lansoprazole and pantoprazole with P-glycoprotein. Naunyn-Schmiedeberg's archives of pharmacology. 2001. Pauli-Magnus C, et al. PubMed
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The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. The Journal of clinical investigation. 1999. Greiner B, et al. PubMed
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Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Annual review of pharmacology and toxicology. 1999. Ambudkar S V, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Competitive, non-competitive and cooperative interactions between substrates of P-glycoprotein as measured by its ATPase activity. Biochimica et biophysica acta. 1997. Litman T, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Unusual Rel-like architecture in the DNA-binding domain of the transcription factor NFATc. Nature. 1997. Wolfe S A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Mode of action of tacrolimus (FK506): molecular and cellular mechanisms. Therapeutic drug monitoring. 1995. Thomson A W, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
P-glycoprotein structure and evolutionary homologies. Cytotechnology. 1993. Croop J M. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
FK-506, a novel immunosuppressant isolated from a Streptomyces. II. Immunosuppressive effect of FK-506 in vitro. The Journal of antibiotics. 1987. Kino T, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0469-0607-73
DrugBank:
DB00864
PDB:
FK5
ChEBI:
61049
KEGG Compound:
C01375
PubChem Compound:
439492
445647
PubChem Substance:
4572
46506004
Drugs Product Database (DPD):
2243144
HET:
FK5
Therapeutic Targets Database:
DAP000162
FDA Drug Label at DailyMed:
7f667de1-9dfa-4bd6-8ba0-15ee2d78873b

Clinical Trials

These are trials that mention tacrolimus and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.