Drug/Small Molecule:
tamoxifen

last updated 08/10/2011

Dutch Pharmacogenetics Working Group Guideline for tamoxifen and CYP2D6

Summary

For CYP2D6 poor and intermediate metabolizers, consider using aromatase inhibitors for postmenopausal women due to increased risk for relapse of breast cancer with tamoxifen. For intermediate metabolizers, avoid concomitant CYP2D6 inhibitor use.

Annotation

The Royal Dutch Pharmacists Association - Pharmacogenetics Working Group has evaluated therapeutic dose recommendations for tamoxifen based on CYP2D6 genotypes (PMID:21412232). For PM and IM genotypes, they recommend considering using aromatase inhibitors for postmenopausal women due to increased risk for relapse of breast cancer with tamoxifen. For IM genotypes, they recommend avoiding concomitant CYP2D6 inhibitor use.

Phenotype (Genotype) Therapeutic Dose Recommendation Level of Evidence Clinical Relevance
PM (two inactive (*3-*8, *11-*16, *19-*21, *38, *40, *42) alleles) Increased risk for relapse of breast cancer. Consider aromatase inhibitor for postmenopausal women. 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): Failure of lifesaving therapy e.g. anticipated myelosuppression; prevention of breast cancer relapse; arrhythmia; neutropenia < 0.5x109/l; leucopenia < 1.0x109/l; thrombocytopenia < 25x109/l; life-threatening complications from diarrhea.
IM (two decreased-activity (*9, *10, *17, *29, *36, *41) alleles or carrying one active (*1, *2, *33, *35) and one inactive (*3-*8, *11-*16, *19-*21, *38, *40, *42) allele, or carrying one decreased-activity (*9, *10, *17, *29, *36, *41) allele and one inactive (*3-*8, *11-*16, *19-*21, *38, *40, *42) allele) Increased risk for relapse of breast cancer. Avoid concomitant use of CYP2D6 inhibitors. Consider aromatase inhibitor for postmenopausal women. 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): Failure of lifesaving therapy e.g. anticipated myelosuppression; prevention of breast cancer relapse; arrhythmia; neutropenia < 0.5x109/l; leucopenia < 1.0x109/l; thrombocytopenia < 25x109/l; life-threatening complications from diarrhea.
UM (a gene duplication in absence of inactive (*3-*8, *11-*16, *19-*21, *38, *40, *42) or decreased-activity (*9, *10, *17, *29, *36, *41) alleles) No. Published controlled studies of good quality* relating to phenotyped and/or genotyped patients or healthy volunteers, and having relevant pharmacokinetic or clinical endpoints. Minor clinical effect (S): QTc prolongation (<450 ms female, <470 ms male); INR increase < 4.5. Kinetic effect (S).

PharmGKB gathers information regarding PGx on FDA drug labels from the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels", and from FDA-approved FDA and EMA-approved (European Medicines Agency) EMA labels brought to our attention. Excerpts from the label and downloadable highlighted label PDFs are manually curated by PharmGKB.

Please note that some drugs may have been removed from or added to the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels" without our knowledge. We periodically check the table for additions to this table and update PharmGKB accordingly.

There is currently no such list for European drug labels - we are working with the EMA to establish a list of European Public Assessment Reports (EPAR)s that contain PGx information. We are constructing this list by initially searching for drugs for which we have PGx-containing FDA drug labels - of these 44 EMA EPARs were identified and are being curated for pgx information.

We welcome any information regarding drug labels containing PGx information approved by the FDA, EMA or other Medicine Agencies around the world - please contact feedback.


last updated 01/16/2014

FDA Label for tamoxifen and ESR1, ESR2, F2, F5

This label is on the FDA Biomarker List
Actionable PGx

Summary

Tamoxifen is an anti-estrogen used in the treatment and prevention of breast neoplasms particularly those with estrogen receptor positive breast cancer.

Annotation

Tamoxifen is an anti-estrogen used in the treatment and prevention of breast neoplasms particularly those with estrogen receptor positive breast cancer.

Excerpts from the tamoxifen (Nolvadex) drug label:

Available evidence indicates that patients whose tumors are estrogen receptor positive are more likely to benefit from NOLVADEX therapy.

The estrogen and progesterone receptor values may help to predict whether adjuvant NOLVADEX therapy is likely to be beneficial. NOLVADEX reduces the occurrence of contralateral breast cancer in patients receiving adjuvant NOLVADEX therapy for breast cancer.

The FDA also highlight factor V Leiden and Prothrombin mutations in their "Table of Pharmacogenomic Biomarkers in Drug Labels", however in the trial mentioned within the drug label there was no benefit of screening for these factors:

When NOLVADEX is coadminstered with chemotherapy, there may be a further increase in the incidence of thromboembolic effects. For treatment of breast cancer, the risks and benefits of NOLVADEX should be carefully considered in women with a history of thromboembolic events. In a subsmall study (N=81) of the NSABP P-1 trial, there appeared to be no benefit to screening women for Factor V Leiden and Prothrombin mutations G20210A as a means to identify those who may not be appropriate candidates for NOLVADEX therapy.

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the tamoxifen drug label.

*Disclaimer: The contents of this page have not been endorsed by the FDA and are the sole responsibility of PharmGKB.

Full label available at DailyMed

Genes and/or phenotypes found in this label

  • Breast Neoplasms
    • Indications & usage section, Contraindications section, Warnings section, Adverse reactions section, Precautions section
    • source: PHONT
  • Death
    • Warnings section, Adverse reactions section, Precautions section
    • source: PHONT
  • Depression
    • Adverse reactions section
    • source: PHONT
  • Hot Flashes
    • Adverse reactions section
    • source: PHONT
  • Neoplasms
    • Indications & usage section, Contraindications section, Warnings section, Adverse reactions section, Precautions section
    • source: PHONT
  • Pain
    • Warnings section, Adverse reactions section, Precautions section
    • source: PHONT
  • ESR1
    • Indications & usage section, Precautions section, efficacy
    • source: FDA Label
  • ESR2
    • Indications & usage section, Precautions section, efficacy
    • source: FDA Label
  • F2
    • Warnings section, toxicity
    • source: FDA Label
  • F5
    • Warnings section, toxicity
    • source: FDA Label

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

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.

? = Mouse-over for quick help

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?
Roche AmpliChip CYP450 Test CYP2D6*1, CYP2D6*10A, CYP2D6*10B, CYP2D6*11, CYP2D6*15, CYP2D6*17, CYP2D6*19, CYP2D6*20, CYP2D6*29, CYP2D6*2A, CYP2D6*2B, CYP2D6*2D, CYP2D6*3, CYP2D6*40, CYP2D6*41, CYP2D6*4A, CYP2D6*4B, CYP2D6*4D, CYP2D6*4J, CYP2D6*4K, CYP2D6*5, CYP2D6*6A, CYP2D6*6B, CYP2D6*6C, CYP2D6*7, CYP2D6*8, CYP2D6*9 , CYP2D6*1XN , CYP2D6*2XN , CYP2D6*4XN , CYP2D6*10XN , CYP2D6*17XN , CYP2D6*35XN , CYP2D6*41XN , *35 , *36
GenoChip CYP2D6 (PharmGenomics, GmbH) CYP2D6*5 , rs59421388 , rs28371725 , rs5030867 , rs5030656 , rs35742686 , rs3892097 , rs5030865 , rs5030655 , rs28371706 , rs5030863 , rs1065852 , *xN (gene duplication)

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.

Gene ? Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No VIP available VA CYP2C19 *1A N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *2A N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *17 N/A N/A N/A
VIP CA VA CYP2D6 *1 N/A N/A N/A
VIP No VIP available No VIP available CYP2D6 *2 N/A N/A N/A
VIP CA VA CYP2D6 *3 N/A N/A N/A
VIP CA VA CYP2D6 *4 N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *4A N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *4D N/A N/A N/A
No VIP available CA VA CYP2D6 *5 N/A N/A N/A
VIP CA VA CYP2D6 *6 N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *6B N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *7 N/A N/A N/A
VIP No VIP available No VIP available CYP2D6 *9 N/A N/A N/A
VIP CA VA CYP2D6 *10 N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *11 N/A N/A N/A
VIP No VIP available VA CYP2D6 *17 N/A N/A N/A
VIP No VIP available No VIP available CYP2D6 *29 N/A N/A N/A
VIP CA VA CYP2D6 *41 N/A N/A N/A
No VIP available No VIP available VA SULT1A1 *1 N/A N/A N/A
No VIP available No VIP available VA SULT1A1 *2 N/A N/A N/A
No VIP available CA VA
rs10030044 157011923G>T, 81559644G>T
G > T
Not Available
No VIP available CA VA
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 No Clinical Annotations available VA
rs10509373 28962036T>C, 517+73329T>C, 78157572T>C
T > C
Intronic
rs1065852 100C>T, 21917263G>A, 42526694G>A, 5190C>T, CYP2D6:100C>T, Pro34Ser, part of CYP2D6*4 and CYP2D6*10
G > A
Missense
Pro34Ser
No VIP available No Clinical Annotations available VA
rs11023197 -1319C>T, -1338C>T, -582, -582C>T, 10055C>T, 14320998G>A, 14380998G>A, 3+4939C>T, 417536G>A, RRAS2, RRAS2:, TC21
G > A
5' Flanking
No VIP available No Clinical Annotations available VA
rs1135840 1304G>G, 1457G>G, 21913182G>C, 42522613G>C, 9271G>G, CYP2D6: S486T, CYP2D6:4180G>C, Ser435=, Ser486=, part of CYP2D6*2A an extensive metabolizer haplotype.
G > C
Missense
Ser435Thr
No VIP available No Clinical Annotations available VA
rs12248560 -806C>A, -806C>T, 4195C>A, 4195C>T, 47326121C>A, 47326121C>T, 96521657C>A, 96521657C>T, CYP2C19*17, CYP2C19*17 CYP2C19: -806C>T, CYP2C19: -806C>T
C > T
C > A
5' Flanking
rs16947 21914512A>G, 42523943A>G, 733C>C, 7941C>C, 886C>C, Arg245=, Arg296=, CYP2D6:2850C>T
A > G
Not Available
No VIP available No Clinical Annotations available VA
rs1801123 227661043T>C, 2412A>G, 7464A>G, 77870461T>C, Ala804=
T > C
Synonymous
Ala804Ala
No VIP available No Clinical Annotations available VA
rs1804645 172613C>T, 24974958C>T, 3796845C>T, 3814C>T, Pro1272Ser
C > T
Missense
Pro1272Ser
No VIP available No Clinical Annotations available VA
rs2011425 134219T>G, 142T>G, 234627608T>G, 573867T>G, 60+25097T>G, 855+36170T>G, 855+46173T>G, 856-48072T>G, 861+25097T>G, 867+5104T>G, Leu48Val
T > G
Intronic
Leu48Val
No VIP available No Clinical Annotations available VA
rs2016347 *3129G>T, 14469327G>T, 316040G>T, 99503800G>T
G > T
3' UTR
No VIP available No Clinical Annotations available VA
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 > C
A > T
Missense
Ser893Ala
Ser893Thr
No VIP available No Clinical Annotations available VA
rs2273697 101563815G>A, 1249G>A, 26353G>A, 52368279G>A, ABCC2: c.1249G>A, ABCC2:1249G>A, ABCC2:V417I, ABCC2:c.1249G>A, Val417Ile, p.V417I
G > A
Missense
Val417Ile
No VIP available No Clinical Annotations available 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
rs28371706 21916341G>A, 320C>T, 42525772G>A, 6112C>T, CYP2D6:1023 C>T, Thr107Ile
G > A
Missense
Thr107Ile
rs28371725 21914374C>T, 42523805C>T, 8079G>A, 832+39G>A, 985+39G>A, CYP2D6*41, CYP2D6:2988G>A, part of CYP2D6*41
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs2854744 -336C>A, 45951075G>T, 45961075G>T, 4797C>A
G > T
5' Flanking
No VIP available No Clinical Annotations available VA
rs2946834 102787814A>G, 64931120A>G, 91565T>C
A > G
Not Available
No VIP available No Clinical Annotations available VA
rs310786 1123+697G>A, 39579454C>T, 77436148C>T
C > T
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
rs35742686 -1793delT, -1830delT, -1940delT, 23418678delT, 40+2664delT, 42128242delT, 50569delT, 50583delT, 598delA, 622delA, 6750delA, 775delA, Arg200Glyfs, Arg208Glyfs, Arg259Glyfs
T > -
Not Available
Arg208Gly
No VIP available No Clinical Annotations available VA
rs3732219 -219C>T, 133859C>T, 234627248C>T, 573507C>T, 60+24737C>T, 855+35810C>T, 855+45813C>T, 856-48432C>T, 861+24737C>T, 867+4744C>T
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs3740065 101605693A>G, 4146+154A>G, 52410157A>G, 68231A>G
A > G
Intronic
rs3892097 21915516C>T, 353-1G>A, 42524947C>T, 506-1G>A, 6937G>A, CYP2D6*4, CYP2D6:1846G>A, part of CYP2D6*4
C > T
Acceptor
No VIP available No Clinical Annotations available VA
rs4244285 24154G>A, 24154G>C, 47346080G>A, 47346080G>C, 681G>A, 681G>C, 96541616G>A, 96541616G>C, CYP2C19*2, CYP2C19:681G>A, CYP2C19:G681A, Pro227=
G > C
G > A
Synonymous
Pro227Pro
No VIP available No Clinical Annotations available VA
rs478437 144793834C>T, 5389457C>T
C > T
Not Available
No VIP available CA VA
rs4986938 *39G>A, 110453G>A, 1406+1872G>A, 45699816C>T, 64699816C>T, ESR2-02, ESR2:1730A>G, ESR2:rs4986938
C > T
Not Available
rs5030655 -1098delA, -1563delA, -951delA, -988delA, 23419520delA, 277delT, 353-140delT, 40+3506delA, 42129084delA, 454delT, 51411delA, 51425delA, 5908delT, CYP2D6*6, CYP2D6:1707 del T, Trp152Glyfs, Trp93Glyfs, part of CYP2D6*6
A > -
Not Available
Trp152Gly
rs5030656 21914745_21914747delCTT, 42524176_42524178delCTT, 688_690delAAG, 7706_7708delAAG, 841_843delAAG, Lys230del, Lys281del
CTT > -
CTT > TTC
Non-synonymous
rs59421388 1012G>A, 21914179C>T, 3271G>A, 42523610C>T, 8274G>A, 859G>A, CYP2D6: 3183G>A, Val287Met, Val338Met
G > T
G > C
Missense
Val287Met
VIP No Clinical Annotations available No Variant Annotations available
rs6025 1601G>A, 1601G>G, 169519049T>C, 169519049T>T, 21007691T>C, 21007691T>T, 41721G>A, 41721G>G, Arg534=, Arg534Gln, F5:Factor V Leiden
T > C
Missense
Arg534Gln
VIP No Clinical Annotations available No Variant Annotations available
rs61736512 1747G>A, 21915703C>T, 353-188G>A, 406G>A, 42525134C>T, 6750G>A, CYP2D6: 1659G>A, Val136Met
G > T
G > C
Intronic
Val136Met
No VIP available No Clinical Annotations available VA
rs6214 *2716G>A, *2750G>A, 102793569C>T, 64936875C>T, 85810G>A
C > T
3' UTR
No VIP available No Clinical Annotations available VA
rs6755571 134147C>A, 234627536C>A, 573795C>A, 60+25025C>A, 70C>A, 855+36098C>A, 855+46101C>A, 856-48144C>A, 861+25025C>A, 867+5032C>A, Pro24Thr
C > A
Intronic
Pro24Thr
No VIP available No Clinical Annotations available VA
rs7136446 102838515C>T, 173-25047G>A, 221-25047G>A, 40864G>A, 64981821C>T
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs717620 -24C>T, 101542578C>T, 5116C>T, 52347042C>T, ABCC2: 5'UTR, ABCC2:(-24)C>T, mRNA 118C>T
C > T
5' UTR
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 CA VA
rs8060157 -164-6747T>C, 17-6747T>C, 3444403A>G, 49830204A>G, 66627T>C
A > G
Intronic
No VIP available No Clinical Annotations available VA
rs8330 *440G>C, 188256G>C, 234681645G>C, 627904G>C
G > C
3' UTR
No VIP available No Clinical Annotations available VA
rs9282861 22353G>A, 28557514C>T, 28617514C>T, 404G>A, 638G>A, Arg135His, Arg213His, SULT1A1*2, SULT1A1:638G>A:SULT1A1:Arg213His
C > T
Not Available
Arg213His
No VIP available CA VA
rs9340799 152163381A>G, 156751A>G, 453-351A>G, 56332838A>G, ESR1:XbaI, ESR1:c.454-351A>G, ESR1:rs9340799
A > G
Intronic
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Tamoxifen Citrate
  • Tamoxifene [INN-French]
  • Tamoxifeno [INN-Spanish]
  • Tamoxifenum [INN-Latin]
  • Trans-Tamoxifen
Trade Names
  • Apo-Tamox
  • Citofen
  • Crisafeno
  • Diemon
  • Gen-Tamoxifen
  • Istubol
  • Kessar
  • Noltam
  • Nolvadex
  • Nolvadex-D
  • Nourytam
  • Novo-Tamoxifen
  • Oncomox
  • PMS-Tamoxifen
  • Retaxim
  • Tamizam
  • Tamofen
  • Tamone
  • Tamoxasta
  • Tamoxen
  • Valodex
  • Zemide
Brand Mixture Names

PharmGKB Accession Id:
PA451581

Description

One of the selective estrogen receptor modulators with tissue-specific activities. Tamoxifen acts as an anti-estrogen (inhibiting agent) in the mammary tissue, but as an estrogen (stimulating agent) in cholesterol metabolism, bone density, and cell proliferation in the endometrium.

Source: Drug Bank

Indication

For the treatment of breast cancer.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Tamoxifen binds to estrogen receptors (ER), inducing a conformational change in the receptor. This results in a blockage or change in the expression of estrogen dependent genes. The prolonged binding of tamoxifen to the nuclear chromatin of these results in reduced DNA polymerase activity, impaired thymidine utilization, blockade of estradiol uptake, and decreased estrogen response. It is likely that tamoxifen interacts with other coactivators or corepressors in the tissue and binds with different estrogen receptors, ER-alpha or ER-beta, producing both estrogenic and antiestrogenic effects.

Source: Drug Bank

Pharmacology

Tamoxifen belongs to a class of drugs called selective estrogen receptor modulators (SERMs), which have both estrogenic and antiestrogenic effects. Tamoxifen has the same nucleus as diethylstilbestrol but possesses an additional side chain (trans isomer) which accounts for its antiestrogenic activity.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. Tamoxifen is extensively metabolized after oral administration. N-Desmethyl-tamoxifen is the major metabolite found in plasma. N-Desmethyl-tamoxifen activity is similar to tamoxifen. 4-hydroxy-tamoxifen and a side chain primary alcohol derivative of tamoxifen have been identified as minor metabolites in plasma. 4-Hydroxy-tamoxifen formation is catalyzed mainly by cytochrome P450 (CYP) 2D6, and also by CYP2C9 and 3A4. At high tamoxifen concentrations, CYP2B6 also catalyzes 4-hydroxylation of the parent drug. 4-Hydroxy-tamoxifen possesses 30- to 100-times greater affinity for the estrogen receptor and 30- to 100-times greater potency at inhibiting estrogen-dependent cell proliferation compared to tamoxifen.

Source: Drug Bank

Half-Life

Distribution t 1/2=7 to 14 hours; Elimination t 1/2=5 to 7 days; Elimination t 1/2 of N-desmethyl-tamoxifen=9-14 days.

Source: Drug Bank

Toxicity

Signs observed at the highest doses following studies to determine LD 50 in animals were respiratory difficulties and convulsions.

Source: Drug Bank

Route of Elimination

The drug is excreted mainly as polar conjugates, with unchanged drug and unconjugated metabolites accounting for less than 30% of the total fecal radioactivity.

Source: Drug Bank

Chemical Properties

Chemical Formula

C26H29NO

Source: Drug Bank

Isomeric SMILES

CC/C(=C(\c1ccccc1)/c2ccc(cc2)OCCN(C)C)/c3ccccc3

Source: OpenEye

Canonical SMILES

CC\C(=C(/C1=CC=CC=C1)C1=CC=C(OCCN(C)C)C=C1)C1=CC=CC=C1

Source: Drug Bank

Average Molecular Weight

371.5146

Source: Drug Bank

Monoisotopic Molecular Weight

371.224914555

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Tamoxifen Pathway, Pharmacokinetics
    Tamoxifen metabolism in the liver.

External Pathways

Links to non-PharmGKB pathways.

  1. FMO oxidizes nucleophiles - (Reactome via Pathway Interaction Database)
  2. telomeres telomerase cellular aging and immortality - (BioCarta via Pathway Interaction Database)

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
ABCB1 (source: Drug Bank)
EPHX2 (source: Drug Bank)
ESR1 (source: Drug Bank)
ESR2 (source: Drug Bank)
TYMP (source: Drug Bank)

Drug Interactions

Drug Description
tamoxifen Decreases the effect of tamoxifen (source: Drug Bank)
tamoxifen Aminoglutethimide may decrease the effect of tamoxifen. (source: Drug Bank)
tamoxifen This combination presents an increased risk of toxicity (source: Drug Bank)
tamoxifen The rifamycin decreases the effect of anti-estrogen (source: Drug Bank)
tamoxifen The rifamycin decreases the effect of anti-estrogen (source: Drug Bank)
tamoxifen The rifamycin decreases the effect of anti-estrogen (source: Drug Bank)
tamoxifen The rifamycin decreases the effect of anti-estrogen (source: Drug Bank)
acenocoumarol Tamoxifen may increase the serum concentration of Acenocoumarol increasing the risk of bleeding. Concomitant therapy should be avoided. (source: Drug Bank)
acenocoumarol Tamoxifen may increase the serum concentration of Acenocoumarol increasing the risk of bleeding. Concomitant therapy should be avoided. (source: Drug Bank)
aminoglutethimide Aminoglutethimide may increase Tamoxifen clearance decreasing its therapeutic effect. Consider alternate therapy or monitor for changes in Tamoxifen effects when Aminoglutethimide is initiated, discontinued or dose changed. (source: Drug Bank)
aminoglutethimide Aminoglutethimide may increase Tamoxifen clearance decreasing its therapeutic effect. Consider alternate therapy or monitor for changes in Tamoxifen effects when Aminoglutethimide is initiated, discontinued or dose changed. (source: Drug Bank)
amiodarone Amiodarone may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
amiodarone Amiodarone may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
amprenavir Amprenavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
amprenavir Amprenavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
atazanavir Atazanavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
atazanavir Atazanavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
capecitabine Capecitabine may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Capecitabine is initiated, discontinued or dose changed. (source: Drug Bank)
capecitabine Capecitabine may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Capecitabine is initiated, discontinued or dose changed. (source: Drug Bank)
chloroquine Chloroquine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
chloroquine Chloroquine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
chlorpromazine Chlorpromazine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
chlorpromazine Chlorpromazine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
cimetidine Cimetidine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
cimetidine Cimetidine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
cinacalcet Cinacalcet may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
cinacalcet Cinacalcet may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
clarithromycin Clarithromycin may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
clarithromycin Clarithromycin may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
clomipramine Clomipramine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
clomipramine Clomipramine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
clozapine Clozapine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
clozapine Clozapine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
cocaine Cocaine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
cocaine Cocaine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
conivaptan Conivaptan may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
conivaptan Conivaptan may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
darifenacin Darifenacin may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
darifenacin Darifenacin may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
darunavir Darunavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
darunavir Darunavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
delavirdine Delavirdine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
delavirdine Delavirdine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
desipramine Desipramine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
desipramine Desipramine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
diphenhydramine Diphenhydramine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
diphenhydramine Diphenhydramine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
duloxetine Duloxetine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
duloxetine Duloxetine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
floxuridine Floxuridine may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Floxiridine is initiated, discontinued or dose changed. (source: Drug Bank)
floxuridine Floxuridine may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Floxiridine is initiated, discontinued or dose changed. (source: Drug Bank)
fluconazole Fluconzole may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Fluconazole is initiated, discontinued or dose changed. (source: Drug Bank)
fluconazole Fluconzole may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Fluconazole is initiated, discontinued or dose changed. (source: Drug Bank)
fluorouracil Fluorouracil may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Fluorouracil is initiated, discontinued or dose changed. (source: Drug Bank)
fluorouracil Fluorouracil may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Fluorouracil is initiated, discontinued or dose changed. (source: Drug Bank)
fluoxetine Fluoxetine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
fluoxetine Fluoxetine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
flurbiprofen Flurbiprofen may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Flurbiprofen is initiated, discontinued or dose changed. (source: Drug Bank)
flurbiprofen Flurbiprofen may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Flurbiprofen is initiated, discontinued or dose changed. (source: Drug Bank)
fosamprenavir Fosmprenavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
fosamprenavir Fosmprenavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
gemfibrozil Gemfibrozil may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Gemfibrozil is initiated, discontinued or dose changed. (source: Drug Bank)
gemfibrozil Gemfibrozil may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Gemfibrozil is initiated, discontinued or dose changed. (source: Drug Bank)
haloperidol Haloperidol may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
haloperidol Haloperidol may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
ibuprofen Ibuprofen may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Ibuprofen is initiated, discontinued or dose changed. (source: Drug Bank)
ibuprofen Ibuprofen may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Ibuprofen is initiated, discontinued or dose changed. (source: Drug Bank)
imatinib Imatinib may increase the serum concentration of Tamoxifen by decreasing its metabolism and clearance. Imatinib may also decrease the therapeutic effect of Tamoxifen by decreasing active metabolite production. Monitor for changes in the therapeutic/adverse effects of Tamoxifen if Imatinib is initiated, discontinued or dose changed. (source: Drug Bank)
imatinib Imatinib may increase the serum concentration of Tamoxifen by decreasing its metabolism and clearance. Imatinib may also decrease the therapeutic effect of Tamoxifen by decreasing active metabolite production. Monitor for changes in the therapeutic/adverse effects of Tamoxifen if Imatinib is initiated, discontinued or dose changed. (source: Drug Bank)
imipramine Imipramine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
imipramine Imipramine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
indinavir Indinavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
indinavir Indinavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
indomethacin Indomethacin may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Indomethacin is initiated, discontinued or dose changed. (source: Drug Bank)
indomethacin Indomethacin may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Indomethacin is initiated, discontinued or dose changed. (source: Drug Bank)
isoniazid Isoniazid may increase the serum concentration of Tamoxifen by decreasing its metabolism and clearance. Isoniazid may also decrease the therapeutic effect of Tamoxifen by decreasing active metabolite production. Monitor for changes in the therapeutic/adverse effects of Tamoxifen if Isoniazid is initiated, discontinued or dose changed. (source: Drug Bank)
isoniazid Isoniazid may increase the serum concentration of Tamoxifen by decreasing its metabolism and clearance. Isoniazid may also decrease the therapeutic effect of Tamoxifen by decreasing active metabolite production. Monitor for changes in the therapeutic/adverse effects of Tamoxifen if Isoniazid is initiated, discontinued or dose changed. (source: Drug Bank)
itraconazole Itraconazole may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
itraconazole Itraconazole may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
ketoconazole Ketoconazole may increase the serum concentration of Tamoxifen by decreasing its metabolism and clearance. Ketoconazole may also decrease the therapeutic effect of Tamoxifen by decreasing active metabolite production. Monitor for changes in the therapeutic/adverse effects of Tamoxifen if Ketoconazole is initiated, discontinued or dose changed. (source: Drug Bank)
ketoconazole Ketoconazole may increase the serum concentration of Tamoxifen by decreasing its metabolism and clearance. Ketoconazole may also decrease the therapeutic effect of Tamoxifen by decreasing active metabolite production. Monitor for changes in the therapeutic/adverse effects of Tamoxifen if Ketoconazole is initiated, discontinued or dose changed. (source: Drug Bank)
lidocaine Lidocaine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
lidocaine Lidocaine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
lopinavir Lopinavir may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
lopinavir Lopinavir may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
methadone Methadone may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
methadone Methadone may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
methimazole Methimazole may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
methimazole Methimazole may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
miconazole Miconazole may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
miconazole Miconazole may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
nefazodone Nefazodone may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
nefazodone Nefazodone may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
nelfinavir Nelfinavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
nelfinavir Nelfinavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
nicardipine Nicardipine may increase the serum concentration of Tamoxifen by decreasing its metabolism and clearance. Nicardipine may also decrease the therapeutic effect of Tamoxifen by decreasing active metabolite production. Monitor for changes in the therapeutic/adverse effects of Tamoxifen if Nicardipine is initiated, discontinued or dose changed. (source: Drug Bank)
nicardipine Nicardipine may increase the serum concentration of Tamoxifen by decreasing its metabolism and clearance. Nicardipine may also decrease the therapeutic effect of Tamoxifen by decreasing active metabolite production. Monitor for changes in the therapeutic/adverse effects of Tamoxifen if Nicardipine is initiated, discontinued or dose changed. (source: Drug Bank)
nilotinib Nilotinib may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
nilotinib Nilotinib may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
paroxetine Paroxetine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
paroxetine Paroxetine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
pergolide Pergolide may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
pergolide Pergolide may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
pioglitazone Pioglitazone may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
pioglitazone Pioglitazone may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
piroxicam Piroxicam may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Piroxicam is initiated, discontinued or dose changed. (source: Drug Bank)
piroxicam Piroxicam may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Piroxicam is initiated, discontinued or dose changed. (source: Drug Bank)
posaconazole Posaconazole may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
posaconazole Posaconazole may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
pyrimethamine Pyrimethamine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
pyrimethamine Pyrimethamine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
quinidine Quinidine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
quinidine Quinidine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
quinine Quinine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
quinine Quinine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
ranolazine Ranolazine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
ranolazine Ranolazine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
ritonavir Ritonavir may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
ritonavir Ritonavir may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
saquinavir Saquinavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
saquinavir Saquinavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
sertraline Sertraline may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
sertraline Sertraline may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
sulfadiazine Sulfadiazine may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Sulfadiazine is initiated, discontinued or dose changed. (source: Drug Bank)
sulfadiazine Sulfadiazine may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Sulfadiazine is initiated, discontinued or dose changed. (source: Drug Bank)
sulfisoxazole Sulfisoxazole may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Sulfisoxazole is initiated, discontinued or dose changed. (source: Drug Bank)
sulfisoxazole Sulfisoxazole may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Sulfisoxazole is initiated, discontinued or dose changed. (source: Drug Bank)
telithromycin Telithromycin may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
telithromycin Telithromycin may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
terbinafine Terbinafine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
terbinafine Terbinafine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
thioridazine Thioridazine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
thioridazine Thioridazine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
ticlopidine Ticlopidine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
ticlopidine Ticlopidine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
tolbutamide Tolbutamide may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Tolbutamide is initiated, discontinued or dose changed. (source: Drug Bank)
tolbutamide Tolbutamide may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Tolbutamide is initiated, discontinued or dose changed. (source: Drug Bank)
topotecan Tamoxifen may increase serum concentrations of oral Topotecan. Concomitant therapy should be avoided. (source: Drug Bank)
topotecan Tamoxifen may increase serum concentrations of oral Topotecan. Concomitant therapy should be avoided. (source: Drug Bank)
tranylcypromine Tranylcypromine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
tranylcypromine Tranylcypromine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
trazodone Trazodone may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
trazodone Trazodone may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
voriconazole Voriconazole may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
voriconazole Voriconazole may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
warfarin Tamoxifen may increase the serum concentration of Warfarin increasing the risk of bleeding. Concomitant therapy should be avoided. (source: Drug Bank)
warfarin Tamoxifen may increase the serum concentration of Warfarin increasing the risk of bleeding. Concomitant therapy should be avoided. (source: Drug Bank)
tamoxifen Telithromycin may reduce clearance of Tamoxifen. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tamoxifen if Telithromycin is initiated, discontinued or dose changed. (source: Drug Bank)
tamoxifen Terbinafine may decrease the efficacy of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
tamoxifen Ticlopidine may decrease the efficacy of Tamoxifen by decreasing the production of active metabolites. Alternate therapy should be considered. (source: Drug Bank)
tamoxifen Tolbutamide, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Tamoxifen. Consider alternate therapy or monitor for changes in Tamoxifen therapeutic and adverse effects if Tolbutamide is initiated, discontinued or dose changed. (source: Drug Bank)
tamoxifen Tolbutamide, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Tamoxifen. Consider alternate therapy or monitor for changes in Tamoxifen therapeutic and adverse effects if Tolbutamide is initiated, discontinued or dose changed. (source: Drug Bank)
tamoxifen The p-glycoprotein inhibitor, Tamoxifen, 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)
tamoxifen The CYP2D6 inhibitor, Tranylcypromine, may decrease the efficacy of Tamoxifen by reducing active metabolite production. Consider alternate therapy. (source: Drug Bank)
tamoxifen The CYP2D6 inhibitor, Trazodone, may decrease the efficacy of Tamoxifen by reducing active metabolite production. Consider alternate therapy. (source: Drug Bank)
tamoxifen The CYP2D6 inhibitor, Trazodone, may decrease the efficacy of Tamoxifen by reducing active metabolite production. Consider alternate therapy. (source: Drug Bank)
tamoxifen The moderate CYP2C8 inhibitor, Tamoxifen, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Tamoxifen is initiated, discontinued to dose changed. (source: Drug Bank)
tamoxifen Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of tamoxifen by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of tamoxifen if voriconazole is initiated, discontinued or dose changed. (source: Drug Bank)
tamoxifen Tamoxifen, a CYP2C9 inhibitor, may increase the serum concentration of warfarin by decreasing its metabolism. Concomitant therapy is contraindicated due to significant increase in bleed risk. (source: Drug Bank)

Curated Information ?

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

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Publications related to tamoxifen: 167

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Profound reduction in the tamoxifen active metabolite endoxifen in a patient on phenytoin for epilepsy compared with a CYP2D6 genotype matched cohort. Pharmacogenetics and genomics. 2014. Gryn Steven E, et al. PubMed
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A Potential Role for Human UDP-glucuronosyltransferase (UGT) 1A4 Promoter SNPs in the Pharmacogenomics of Tamoxifen and its Derivatives. Drug metabolism and disposition: the biological fate of chemicals. 2014. Greer Aleksandra K, et al. PubMed
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PharmGKB summary: very important pharmacogene information for N-acetyltransferase 2. Pharmacogenetics and genomics. 2014. McDonagh Ellen M, et al. PubMed
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Expression profiling of breast cancer patients treated with tamoxifen: prognostic or predictive significance. Medical oncology (Northwood, London, England). 2014. Tabarestani Sanaz, et al. PubMed
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Association between CYP2D6 genotypes and the clinical outcomes of adjuvant tamoxifen for breast cancer: a meta-analysis. Pharmacogenomics. 2014. Jung Jin-A, et al. PubMed
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Patients' Understanding of How Genotype Variation Affects Benefits of Tamoxifen Therapy for Breast Cancer. Public health genomics. 2014. Brewer N T, et al. PubMed
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Decreased expression of Yes-associated protein is associated with outcome in the luminal A breast cancer subgroup and with an impaired tamoxifen response. BMC cancer. 2014. Lehn Sophie, et al. PubMed
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CCNA2 Is a Prognostic Biomarker for ER+ Breast Cancer and Tamoxifen Resistance. PloS one. 2014. Gao Tian, et al. PubMed
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Sox2 promotes tamoxifen resistance in breast cancer cells. EMBO molecular medicine. 2013. Piva Marco, et al. PubMed
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CYP2D6 Genotype and Adjuvant Tamoxifen: Meta-analysis of Heterogeneous Study Populations. Clinical pharmacology and therapeutics. 2013. Province Michael A, et al. PubMed
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Inhibition of cytochrome p450 enzymes by the e- and z-isomers of norendoxifen. Drug metabolism and disposition: the biological fate of chemicals. 2013. Liu Jinzhong, et al. PubMed
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CYP2D6 genotype and tamoxifen activity: understanding interstudy variability in methodological quality. Clinical pharmacology and therapeutics. 2013. Ratain M J, et al. PubMed
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PharmGKB summary: tamoxifen pathway, pharmacokinetics. Pharmacogenetics and genomics. 2013. Klein Daniel J, et al. PubMed
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Selective Estrogen Receptor Modulators and Pharmacogenomic Variation in ZNF423 Regulation of BRCA1 Expression: Individualized Breast Cancer Prevention. Cancer discovery. 2013. Ingle James N, et al. PubMed
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Synthesis of mixed (E,Z)-, (E)-, and (Z)-norendoxifen with dual aromatase inhibitory and estrogen receptor modulatory activities. Journal of medicinal chemistry. 2013. Lv Wei, et al. PubMed
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Implications of Genome-Wide Association Studies in Cancer Therapeutics. British journal of clinical pharmacology. 2013. Patel Jai 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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Mammographic breast density response to aromatase inhibition. Clinical cancer research : an official journal of the American Association for Cancer Research. 2013. Vachon Celine M, et al. PubMed
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CYP2D6 and adjuvant tamoxifen: possible differences of outcome in pre- and post-menopausal patients. Pharmacogenomics. 2013. Margolin Sara, et al. PubMed
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Genome-wide discovery of genetic variants affecting tamoxifen sensitivity and their clinical and functional validation. Annals of oncology : official journal of the European Society for Medical Oncology / ESMO. 2013. Weng L, et al. PubMed
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Insulin-like growth factor receptor polymorphism defines clinical outcome in estrogen receptor-positive breast cancer patients treated with tamoxifen. The pharmacogenomics journal. 2013. Winder T, et al. PubMed
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CYP2D6 Metabolism and Patient Outcome in the Austrian Breast and Colorectal Cancer Study Group Trial (ABCSG) 8. Clinical cancer research : an official journal of the American Association for Cancer Research. 2012. Goetz Matthew P, et al. PubMed
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Laboratory testing of CYP2D6 alleles in relation to tamoxifen therapy. Genetics in medicine : official journal of the American College of Medical Genetics. 2012. Lyon Elaine, et al. PubMed
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ELF5 Suppresses Estrogen Sensitivity and Underpins the Acquisition of Antiestrogen Resistance in Luminal Breast Cancer. PLoS biology. 2012. Kalyuga Maria, et al. PubMed
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Association of CYP3A4/5, ABCB1 and ABCC2 polymorphisms and clinical outcomes of Thai breast cancer patients treated with tamoxifen. Pharmacogenomics and personalized medicine. 2013. Sensorn Insee, et al. PubMed
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Efficacy of histone deacetylase and estrogen receptor inhibition in breast cancer cells due to concerted down regulation of Akt. PloS one. 2013. Thomas Scott, et al. PubMed
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Genetic polymorphisms of CYP2D6 increase the risk for recurrence of breast cancer in patients receiving tamoxifen as an adjuvant therapy. Cancer chemotherapy and pharmacology. 2012. Damodaran Solai Elango, et al. PubMed
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Re: CYP2D6 Genotype and Tamoxifen Response in Postmenopausal Women With Endocrine-Responsive Breast Cancer: The Breast International Group 1-98 Trial. Journal of the National Cancer Institute. 2012. Nakamura Yusuke, 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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Automated discovery of drug treatment patterns for endocrine therapy of breast cancer within an electronic medical record. Journal of the American Medical Informatics Association : JAMIA. 2012. Savova Guergana K, et al. PubMed
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Use of CYP2D6 genotyping in practice: tamoxifen dose adjustment. Pharmacogenomics. 2012. Walko Christine M, et al. PubMed
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Tamoxifen and CYP2D6: A Contradiction of Data. The oncologist. 2012. Hertz Daniel L, et al. PubMed
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A genome-wide association study identifies locus at 10q22 associated with clinical outcomes of adjuvant tamoxifen therapy for breast cancer patients in Japanese. Human molecular genetics. 2012. Kiyotani Kazuma, et al. PubMed
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Arylamine N-acetyltransferase 1: a novel drug target in cancer development. Pharmacological reviews. 2012. Butcher Neville J, et al. PubMed
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Comparison of Changes in the Lipid Profile of Postmenopausal Women With Early Stage Breast Cancer Treated With Exemestane or Letrozole. Journal of clinical pharmacology. 2011. Bell Lauren Nicole, et al. PubMed
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A SNP in Steroid Receptor Coactivator-1 Disrupts a GSK3beta Phosphorylation Site and Is Associated with Altered Tamoxifen Response in Bone. Molecular endocrinology (Baltimore, Md.). 2011. Hartmaier R J, et al. PubMed
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Functional analysis of UGT1A4(P24T) and UGT1A4(L48V) variant enzymes. Pharmacogenomics. 2011. Zhou Jin, et al. PubMed
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Tamoxifen Downregulates Ets Oncogene Family Members ETV4 and ETV5 in Benign Breast Tissue: Implications for Durable Risk Reduction. Cancer prevention research (Philadelphia, Pa.). 2011. Euhus David, et al. PubMed
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Increasing tamoxifen dose in breast cancer patients based on CYP2D6 genotypes and endoxifen levels: effect on active metabolite isomers and the antiestrogenic activity score. Clinical pharmacology and therapeutics. 2011. Barginear M F, et al. PubMed
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SULT1A1, CYP2C19 and disease-free survival in early breast cancer patients receiving tamoxifen. Pharmacogenomics. 2011. Moyer Ann M, et al. PubMed
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Dose-adjustment study of tamoxifen based on CYP2D6 genotypes in Japanese breast cancer patients. Breast cancer research and treatment. 2011. Kiyotani Kazuma, et al. PubMed
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The tamoxifen metabolite norendoxifen is a potent and selective inhibitor of aromatase (CYP19) and a potential lead compound for novel therapeutic agents. Breast cancer research and treatment. 2011. Lu Wenjie Jessie, et al. PubMed
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Evaluation of CYP2D6 and Efficacy of Tamoxifen and Raloxifene in Women Treated for Breast Cancer Chemoprevention: Results from the NSABP P-1 and P-2 Clinical Trials. Clinical cancer research : an official journal of the American Association for Cancer Research. 2011. Goetz Matthew P, et al. PubMed
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Genotype-guided tamoxifen dosing increases active metabolite exposure in women with reduced CYP2D6 metabolism: a multicenter study. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2011. Irvin William J, et al. PubMed
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The CYP2C19*2 genotype predicts tamoxifen treatment outcome in advanced breast cancer patients. Pharmacogenomics. 2011. van Schaik Ron H N, et al. PubMed
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Cancer Pharmacogenomics. Clinical pharmacology and therapeutics. 2011. Paugh S W, et al. PubMed
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Pharmacogenetic testing: time for clinical practice guidelines. Clinical pharmacology and therapeutics. 2011. Amstutz U, et al. PubMed
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Activity Levels of Tamoxifen Metabolites at the Estrogen Receptor and the Impact of Genetic Polymorphisms of Phase I and II Enzymes on Their Concentration Levels in Plasma. Clinical pharmacology and therapeutics. 2011. Mürdter T E, et al. PubMed
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Tamoxifen Metabolite Concentrations, CYP2D6 Genotype, and Breast Cancer Outcomes. Clinical pharmacology and therapeutics. 2011. Madlensky L, et al. PubMed
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Tamoxifen metabolites as active inhibitors of aromatase in the treatment of breast cancer. Breast cancer research and treatment. 2011. Lu Wenjie Jessie, et al. PubMed
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Pharmacogenetics: From Bench to Byte- An Update of Guidelines. Clinical pharmacology and therapeutics. 2011. Swen J J, 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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Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein). Pharmacogenetics and genomics. 2011. Hodges Laura M, et al. PubMed
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Genomics and drug response. The New England journal of medicine. 2011. Wang Liewei, et al. PubMed
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Copy number variants in pharmacogenetic genes. Trends in molecular medicine. 2011. He Yijing, 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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Pharmacogenetic tests in cancer chemotherapy: what physicians should know for clinical application. The Journal of pathology. 2011. Lee Soo-Youn, et al. PubMed
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Pharmacogenomic contribution to drug response. Cancer journal (Sudbury, Mass.). 2011. Watson Roshawn G, et al. PubMed
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Estrogen receptor genotypes, menopausal status, and the effects of tamoxifen on lipid levels: revised and updated results. Clinical pharmacology and therapeutics. 2010. Hayes D F, et al. PubMed
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Impact of CYP2D6*4 genotype on progression free survival in tamoxifen breast cancer treatment. Current medical research and opinion. 2010. Stingl Julia Carolin, et al. PubMed
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Systematic review of pharmacoeconomic studies of pharmacogenomic tests. Pharmacogenomics. 2010. Beaulieu Mathieu, et al. PubMed
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CYP2C19*2 polymorphism is associated with increased survival in breast cancer patients using tamoxifen. Pharmacogenomics. 2010. Ruiter Rikje, et al. PubMed
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PXR-mediated induction of P-glycoprotein by anticancer drugs in a human colon adenocarcinoma-derived cell line. Cancer chemotherapy and pharmacology. 2010. Harmsen Stefan, et al. PubMed
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Expectations, validity, and reality in pharmacogenetics. Journal of clinical epidemiology. 2010. Limdi Nita A, et al. PubMed
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PharmGKB summary: very important pharmacogene information for CYP2B6. Pharmacogenetics and genomics. 2010. Thorn Caroline F, et al. PubMed
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Coprescription of tamoxifen and medications that inhibit CYP2D6. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2010. Sideras Kostandinos, et al. PubMed
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Lessons for pharmacogenomics studies: association study between CYP2D6 genotype and tamoxifen response. Pharmacogenetics and genomics. 2010. Kiyotani Kazuma, et al. PubMed
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Clinical implementation of pharmacogenomics: overcoming genetic exceptionalism. The lancet oncology. 2010. Relling Mary V, et al. PubMed
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Pharmacogenetics of CYP2C19: functional and clinical implications of a new variant CYP2C19*17. British journal of clinical pharmacology. 2010. Li-Wan-Po Alain, et al. PubMed
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Targeted cancer therapies in the twenty-first century: lessons from imatinib. Clinical pharmacology and therapeutics. 2010. Stegmeier F, et al. PubMed
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Nationwide drug-dispensing data reveal important differences in adherence to drug label recommendations on CYP2D6-dependent drug interactions. British journal of clinical pharmacology. 2010. Mannheimer Buster, et al. PubMed
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Composite functional genetic and comedication CYP2D6 activity score in predicting tamoxifen drug exposure among breast cancer patients. Journal of clinical pharmacology. 2010. Borges Silvana, et al. PubMed
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Cytochrome P450 2C9-CYP2C9. Pharmacogenetics and genomics. 2010. Van Booven Derek, et al. PubMed
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Significant effect of polymorphisms in CYP2D6 and ABCC2 on clinical outcomes of adjuvant tamoxifen therapy for breast cancer patients. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2010. Kiyotani Kazuma, et al. PubMed
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Efficacy of tamoxifen based on cytochrome P450 2D6, CYP2C19 and SULT1A1 genotype in the Italian Tamoxifen Prevention Trial. The pharmacogenomics journal. 2010. Serrano D, et al. PubMed
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Lack of association between oestrogen receptor polymorphisms and change in bone mineral density with tamoxifen therapy. British journal of cancer. 2010. Henry N L, et al. PubMed
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Molecular genetics and epigenetics of the cytochrome P450 gene family and its relevance for cancer risk and treatment. Human genetics. 2010. Rodriguez-Antona Cristina, et al. PubMed
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Selective serotonin reuptake inhibitors and breast cancer mortality in women receiving tamoxifen: a population based cohort study. BMJ (Clinical research ed.). 2010. Kelly Catherine M, et al. PubMed
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A pharmacogenetics study of the human glucuronosyltransferase UGT1A4. Pharmacogenetics and genomics. 2009. Benoit-Biancamano Marie-Odile, et al. PubMed
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Pharmacogenetics of breast cancer therapies. Breast (Edinburgh, Scotland). 2009. Hertz Daniel L, et al. PubMed
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Warfarin interactions with substances listed in drug information compendia and in the FDA-approved label for warfarin sodium. Clinical pharmacology and therapeutics. 2009. Anthony M, et al. PubMed
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Association between CYP2D6 polymorphisms and outcomes among women with early stage breast cancer treated with tamoxifen. JAMA : the journal of the American Medical Association. 2009. Schroth Werner, et al. PubMed
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Structure, function, regulation and polymorphism of human cytochrome P450 2A6. Current drug metabolism. 2009. Di Yuan Ming, et al. PubMed
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Substrate specificity, regulation, and polymorphism of human cytochrome P450 2B6. Current drug metabolism. 2009. Mo Sui-Lin, et al. PubMed
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Cytochrome P450 2D6 activity predicts discontinuation of tamoxifen therapy in breast cancer patients. The pharmacogenomics journal. 2009. Rae J M, et al. PubMed
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Clinically available pharmacogenomics tests. Clinical pharmacology and therapeutics. 2009. Flockhart D A, et al. PubMed
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Cytochrome P450 2D6. Pharmacogenetics and genomics. 2009. Owen Ryan P, et al. PubMed
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Estrogen receptor genotype is associated with risk of venous thromboembolism during tamoxifen therapy. Breast cancer research and treatment. 2009. Onitilo Adedayo A, 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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Host genetic variants in the interleukin-6 promoter predict poor outcome in patients with estrogen receptor-positive, node-positive breast cancer. Cancer research. 2009. DeMichele Angela, et al. PubMed
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ADME pharmacogenetics: current practices and future outlook. Expert opinion on drug metabolism & toxicology. 2009. Grossman Iris. 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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Tamoxifen metabolism and its effect on endocrine treatment of breast cancer. Clinical advances in hematology & oncology : H&O. 2009. Briest Susanne, et al. PubMed
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Pharmacogenetics--tailoring treatment for the outliers. The New England journal of medicine. 2009. Woodcock Janet, 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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Pharmacogenetics and pharmacogenomics of anticancer agents. CA: a cancer journal for clinicians. 2009. Huang R Stephanie, et al. PubMed
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A polymorphism in the TC21 promoter associates with an unfavorable tamoxifen treatment outcome in breast cancer. Cancer research. 2008. Rokavec Matjaz, et al. PubMed
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Estrogen receptor genotypes influence hot flash prevalence and composite score before and after tamoxifen therapy. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2008. Jin Yan, et al. PubMed
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Regulation of ERBB2 by oestrogen receptor-PAX2 determines response to tamoxifen. Nature. 2008. Hurtado Antoni, 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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Impaired tamoxifen metabolism reduces survival in familial breast cancer patients. Clinical cancer research : an official journal of the American Association for Cancer Research. 2008. Newman William G, 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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CYP450 pharmacogenetics for personalizing cancer therapy. Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy. 2008. van Schaik Ron H N. PubMed
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Estrogen receptor genotypes, menopausal status, and the lipid effects of tamoxifen. Clinical pharmacology and therapeutics. 2008. Ntukidem N I, et al. PubMed
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Role of human pregnane X receptor in tamoxifen- and 4-hydroxytamoxifen-mediated CYP3A4 induction in primary human hepatocytes and LS174T cells. Drug metabolism and disposition: the biological fate of chemicals. 2008. Sane Rucha S, et al. PubMed
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CYP2D6 phenotype prediction from genotype: which system is the best?. Clinical pharmacology and therapeutics. 2008. Kirchheiner J. PubMed
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Tamoxifen pharmacogenomics: the role of CYP2D6 as a predictor of drug response. Clinical pharmacology and therapeutics. 2008. Goetz M P, 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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Effect of anastrozole and tamoxifen as adjuvant treatment for early-stage breast cancer: 100-month analysis of the ATAC trial. The lancet oncology. 2008. Arimidex, Tamoxifen, Alone or in Combination (ATAC) Trialists' Group, et al. PubMed
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Pharmacogenomics of endocrine therapy in breast cancer. Advances in experimental medicine and biology. 2008. Weinshilboum Richard. PubMed
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Pharmacogenetics and breast cancer endocrine therapy: CYP2D6 as a predictive factor for tamoxifen metabolism and drug response?. Expert reviews in molecular medicine. 2008. Stearns Vered, et al. PubMed
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Influence of cytochrome P450 polymorphisms on drug therapies: pharmacogenetic, pharmacoepigenetic and clinical aspects. Pharmacology & therapeutics. 2007. Ingelman-Sundberg Magnus, et al. PubMed
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Breast cancer treatment outcome with adjuvant tamoxifen relative to patient CYP2D6 and CYP2C19 genotypes. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2007. Schroth Werner, et al. PubMed
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Association between CYP3A4 genotype and risk of endometrial cancer following tamoxifen use. Carcinogenesis. 2007. Chu William, et al. PubMed
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Genetic diversity and function in the human cytosolic sulfotransferases. The pharmacogenomics journal. 2007. Hildebrandt M A T, et al. PubMed
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Reversal of neurological defects in a mouse model of Rett syndrome. Science (New York, N.Y.). 2007. Guy Jacky, et al. PubMed
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The impact of cytochrome P450 2D6 metabolism in women receiving adjuvant tamoxifen. Breast cancer research and treatment. 2007. Goetz Matthew P, et al. PubMed
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Genetic variants of CYP3A5, CYP2D6, SULT1A1, UGT2B15 and tamoxifen response in postmenopausal patients with breast cancer. Breast cancer research : BCR. 2007. Wegman Pia, 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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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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Tamoxifen inhibits cytochrome P450 2C9 activity in breast cancer patients. Journal of chemotherapy (Florence, Italy). 2006. Boruban M C, et al. PubMed
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Endoxifen, a secondary metabolite of tamoxifen, and 4-OH-tamoxifen induce similar changes in global gene expression patterns in MCF-7 breast cancer cells. The Journal of pharmacology and experimental therapeutics. 2006. Lim Young Chai, et al. PubMed
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Quantitative effect of CYP2D6 genotype and inhibitors on tamoxifen metabolism: implication for optimization of breast cancer treatment. Clinical pharmacology and therapeutics. 2006. Borges Silvana, et al. PubMed
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Effect of Factor V Leiden and prothrombin G20210-->A mutations on thromboembolic risk in the national surgical adjuvant breast and bowel project breast cancer prevention trial. Journal of the National Cancer Institute. 2006. Abramson Neil, et al. PubMed
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Ten-year multi-institutional results of breast-conserving surgery and radiotherapy in BRCA1/2-associated stage I/II breast cancer. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2006. Pierce Lori J, 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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Tamoxifen and contralateral breast cancer in BRCA1 and BRCA2 carriers: an update. International journal of cancer. Journal international du cancer. 2006. Gronwald Jacek, 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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Cancer treatment and pharmacogenetics of cytochrome P450 enzymes. Investigational new drugs. 2005. van Schaik Ron H N. PubMed
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Pharmacogenetics of tamoxifen biotransformation is associated with clinical outcomes of efficacy and hot flashes. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2005. Goetz Matthew P, et al. PubMed
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Development and validation of therapeutically relevant multi-gene biomarker classifiers. Journal of the National Cancer Institute. 2005. Simon Richard. PubMed
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CYP2D6 genotype, antidepressant use, and tamoxifen metabolism during adjuvant breast cancer treatment. Journal of the National Cancer Institute. 2005. Jin Yan, et al. PubMed
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The effects of tamoxifen and its metabolites on platelet function and release of reactive oxygen intermediates. The Journal of pharmacology and experimental therapeutics. 2005. Vitseva Olga, et al. PubMed
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Genotype of metabolic enzymes and the benefit of tamoxifen in postmenopausal breast cancer patients. Breast cancer research : BCR. 2005. Wegman Pia, et al. PubMed
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Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. The Journal of pharmacology and experimental therapeutics. 2004. Desta Zeruesenay, et al. PubMed
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Association of breast cancer DNA methylation profiles with hormone receptor status and response to tamoxifen. Cancer research. 2004. Widschwendter Martin, et al. PubMed
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Contralateral breast cancer in BRCA1 and BRCA2 mutation carriers. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2004. Metcalfe Kelly, 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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Pharmacological characterization of 4-hydroxy-N-desmethyl tamoxifen, a novel active metabolite of tamoxifen. Breast cancer research and treatment. 2004. Johnson Michael D, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Interactions of human P-glycoprotein with simvastatin, simvastatin acid, and atorvastatin. Pharmaceutical research. 2004. Hochman Jerome H, 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
Synergistic interactions between tamoxifen and trastuzumab (Herceptin). Clinical cancer research : an official journal of the American Association for Cancer Research. 2004. Argiris Athanassios, 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
Estrogen receptor-mediated regulation of oxidative stress and DNA damage in breast cancer. Carcinogenesis. 2004. Mobley James A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Polymorphisms in human MDR1 (P-glycoprotein): recent advances and clinical relevance. Clinical pharmacology and therapeutics. 2004. Marzolini Catia, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Active tamoxifen metabolite plasma concentrations after coadministration of tamoxifen and the selective serotonin reuptake inhibitor paroxetine. Journal of the National Cancer Institute. 2003. Stearns Vered, 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
Effects of tamoxifen on DNA adduct formation and arylamines N-acetyltransferase activity in human breast cancer cells. Research communications in molecular pathology and pharmacology. 2004. Lee Jau-Hong, 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
Pharmacogenetics in the treatment of breast cancer. The pharmacogenomics journal. 2004. Stearns V, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Inherited and acquired risk factors for venous thromboembolic disease among women taking tamoxifen to prevent breast cancer. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2003. Duggan Catherine, 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
Alpha-hydroxylation of tamoxifen and toremifene by human and rat cytochrome P450 3A subfamily enzymes. Chemical research in toxicology. 2003. Kim Sung Yeon, 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
Involvement of PKA and Sp1 in the induction of p27(Kip1) by tamoxifen. Biochemical pharmacology. 2003. Lee Te-Hsiu, 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
Quantification of tamoxifen and three metabolites in plasma by high-performance liquid chromatography with fluorescence detection: application to a clinical trial. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 2003. Lee Kyung-Hoon, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Genetic polymorphisms of the human MDR1 drug transporter. Annual review of pharmacology and toxicology. 2003. Schwab Matthias, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Association between sulfotransferase 1A1 genotype and survival of breast cancer patients receiving tamoxifen therapy. Journal of the National Cancer Institute. 2002. Nowell Susan, 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
Pharmacokinetics of anastrozole and tamoxifen alone, and in combination, during adjuvant endocrine therapy for early breast cancer in postmenopausal women: a sub-protocol of the 'Arimidex and tamoxifen alone or in combination' (ATAC) trial. British journal of cancer. 2001. Dowsett M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Extensive genetic polymorphism in the human CYP2B6 gene with impact on expression and function in human liver. Pharmacogenetics. 2001. Lang T, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Interaction of omeprazole, lansoprazole and pantoprazole with P-glycoprotein. Naunyn-Schmiedeberg's archives of pharmacology. 2001. Pauli-Magnus C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Tamoxifen and risk of contralateral breast cancer in BRCA1 and BRCA2 mutation carriers: a case-control study. Hereditary Breast Cancer Clinical Study Group. Lancet. 2000. Narod 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
Tamoxifen inhibits arylamine N-acetyltransferase activity and DNA-2-aminofluorene adduct in human leukemia HL-60 cells. Research communications in molecular pathology and pharmacology. 2001. Lu K H, 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
Impact of tamoxifen on the pharmacokinetics and endocrine effects of the aromatase inhibitor letrozole in postmenopausal women with breast cancer. Clinical cancer research : an official journal of the American Association for Cancer Research. 1999. Dowsett M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. The Journal of clinical investigation. 1999. Greiner B, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
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
An intron 1 enhancer element mediates oestrogen-induced suppression of ERBB2 expression. Oncogene. 1997. Bates N P, 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
Anti-oestrogen stimulation of ERBB2 ectodomain shedding from BT-474 human breast cancer cells with ERBB2 gene amplification. European journal of cancer (Oxford, England : 1990). 1996. Wärri A M, 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
Transcriptional repression of the neu protooncogene by estrogen stimulated estrogen receptor. Cancer research. 1992. Russell K S, 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

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0378-0144-91
DrugBank:
DB00675
PDB:
OHT
ChEBI:
9396
KEGG Compound:
C07108
KEGG Drug:
D00966
PubChem Compound:
2733526
PubChem Substance:
46505515
9319
IUPHAR Ligand:
1016
Drugs Product Database (DPD):
2237460
BindingDB:
20607
ChemSpider:
2015313
HET:
OHT
Therapeutic Targets Database:
DAP000108
FDA Drug Label at DailyMed:
7ee3d3d2-85d1-4018-8e70-5ed8a64ae1f0

Clinical Trials

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

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