Drug/Small Molecule:
nelfinavir

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

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 10/25/2013

FDA Label for nelfinavir and CYP2C19, CYP3A

Informative PGx

Summary

Coadministration of VIRACEPT with drugs primarily metabolized by CYP3A may result in increased plasma concentrations of the other drug that could prolong its therapeutic and adverse effects. Coadministration of VIRACEPT and drugs that induce CYP3A or CYP2C19 may decrease nelfinavir plasma concentrations and reduce its therapeutic effect. Coadministration of VIRACEPT and drugs that inhibit CYP3A or CYP2C19 may increase nelfinavir plasma concentrations.

Annotation

The FDA approved drug label for Nelfinavir highlights information regarding metabolism of the drug by CYP3A and CYP2C19, and drugs that inhibit these enzymes may effect nelfinavir's efficacy. The label does not mention pharmacogenetics or genetic testing. This drug-biomarkers pair was previously in the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels" but has subsequently been removed.

Nelfinavir is a protease inhibitor which is used in combination with other medications to treat human immunodeficiency virus (HIV) infection by slowing the spread of the infection within the body. It is metabolized by cytochrome P-450 enzymes, mainly CYP3A and CYP2C19.

Excerpts from the Nelfinavir drug label:

Nelfinavir is an inhibitor of CYP3A. Coadministration of VIRACEPT and drugs primarily metabolized by CYP3A (e.g., dihydropyridine calcium channel blockers, HMG-CoA reductase inhibitors, immunosuppressants and PDE5 inhibitors) may result in increased plasma concentrations of such drugs that could increase or prolong its therapeutic and adverse effects.

Nelfinavir is metabolized by CYP3A and CYP2C19. Coadministration of VIRACEPT and drugs that induce CYP3A or CYP2C19,such as rifampin, may decrease nelfinavir plasma concentrations and reduce its therapeutic effect. Coadministration of VIRACEPT and drugs that inhibit CYP3A or CYP2C19 may increase nelfinavir plasma concentrations.

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

  • HIV
    • Indications & usage section, Precautions section
    • source: PHONT
  • CYP2C19
    • Drug interactions section, Clinical pharmacology section, metabolism/PK
    • source: FDA Label
  • CYP3A
    • Contraindications section, Drug interactions section, Clinical pharmacology section, metabolism/PK
    • source: FDA Label

last updated 10/27/2013

European Medicines Agency (EMA) Label for nelfinavir and CYP3A4

Informative PGx

Summary

The EMA European Public Assessment Report (EPAR) for nelfinavir (Viracept) contains information regarding the metabolism of the drug by CYP3A4, CYP2C19 and CYP2D6, and that concomitant use of CYP3A4 substrates or inducers is contraindicated. No genetic information is included.

Annotation

Excerpt from the nelfinavir (Viracept) EPAR:

Potent inducers of CYP3A4 (e.g., rifampicin, pehnobarbital and carbamazepine) may reduce nelfianvir plasma concentrations and their coadministration is contraindicated (see section 4.3). Caution should be used when co-administering other agents that induce CYP3A4.

Co-administration of nelfinavir with inhibitors of CYP2C19 (e.g., fluconazole, fluoxetine, paroxetine, lansoprazole, imipramine, amitriptyline and diazepam) may be expected to reduce the conversion of nelfinavir to its major active metabolite M8 (tert-butyl hydroxy nelfinavir) with a concomitant increase in plasma nelfinavir levels (see section 5.2). Limited clinical trial data from patients receiving one or more of these medicinal products with nelfinavir indicated that a clinically significant effect on safety and efficacy is not expected. However, such an effect cannot be ruled out.

This information is highlighted in the following sections:
Contraindications, interaction with other medicinal products and other forms of interaction, pharmacodynamic properties.

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the nelfinavir (Viracept) EMA drug label.

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


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?
Spartan RX CYP2C19 System CYP2C19*17, CYP2C19*2, CYP2C19*3 , rs12248560 , rs4986893 , rs4244285

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
VIP No VIP available No VIP available CYP2C19 *2A N/A N/A N/A
VIP No VIP available No VIP available CYP2C19 *3A N/A N/A N/A
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
VIP No Clinical Annotations available No Variant Annotations available
rs1128503 1236T>C, 167964T>C, 25043506A>G, 87550285A>G, ABCB1 1236C>T, ABCB1*8, ABCB1: c.1236T>C, ABCB1:1236C>T, ABCB1:1236T>C, Gly412=, Gly412Gly, mRNA 1654T>C, p.Gly412Gly
A > G
Not Available
Gly412Gly
No VIP available No Clinical Annotations available VA
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
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
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
rs4986893 22948G>A, 47344874G>A, 636G>A, 96540410G>A, CYP2C19*3, CYP2C19:636G>A, CYP2C19:G636A, Trp212Ter
G > A
Stop Codon
Trp212null
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
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • 1UN
  • NFV
  • NLF
  • Nelfinavir mesylate
  • ag1343
Trade Names
  • Viracept
Brand Mixture Names

PharmGKB Accession Id:
PA450606

Description

A potent HIV-1 protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.

Source: Drug Bank

Indication

Used in combination with other antiviral drugs in the treatment of HIV in both adults and children.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Nelfinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.

Source: Drug Bank

Pharmacology

Nelfinavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Nelfinavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs.

Source: Drug Bank

Food Interaction

Food significantly increases absorption (2 to 3 times).|Take with food.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Primarily hepatic via cytochrome P450 (CYP450) enzymes. CYP3A and CYP2C19 appear to be the predominant enzymes that metabolize nelfinavir in humans. One major and several minor metabolites are found in plasma; the major oxidative metabolite has in vitro antiviral activity comparable to that of the parent drug.

Source: Drug Bank

Protein Binding

>98%

Source: Drug Bank

Absorption

Well absorbed following oral administration.

Source: Drug Bank

Half-Life

3.5 - 5 hours

Source: Drug Bank

Toxicity

Oral LD 50 is over 5g/kg in rats. Side effects include thirst and hunger, unexplained weight loss, increased urination, fatigue, and dry, itchy skin.

Source: Drug Bank

Route of Elimination

The terminal half-life in plasma was typically 3.5 to 5 hours. The majority (87%) of an oral 750 mg dose containing 14C-nelfinavir was recovered in the feces; fecal radioactivity consisted of numerous oxidative metabolites (78%) and unchanged nelfinavir (22%). Only 1-2% of the dose was recovered in urine, of which unchanged nelfinavir was the major component.

Source: Drug Bank

Volume of Distribution

  • 2 to 7 L/kg

Source: Drug Bank

Chemical Properties

Chemical Formula

C32H45N3O4S

Source: Drug Bank

Isomeric SMILES

Cc1c(cccc1O)C(=O)N[C@@H](CSc2ccccc2)[C@@H](CN3C[C@H]4CCCC[C@H]4C[C@H]3C(=O)NC(C)(C)C)O

Source: OpenEye

Canonical SMILES

CC1=C(C=CC=C1O)C(=O)N[C@@H](CSC1=CC=CC=C1)[C@H]

Source: Drug Bank

Average Molecular Weight

567.782

Source: Drug Bank

Monoisotopic Molecular Weight

567.313077633

Source: Drug Bank

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

Curated Information ?

Drug Interactions

Drug Description
nelfinavir The serum concentration of Abacavir may be decreased by protease inhibitors such as Nelfinavir. The antiviral response should be closely monitored. (source: Drug Bank)
nelfinavir The serum concentration of Abacavir may be decreased by protease inhibitors such as Nelfinavir. The antiviral response should be closely monitored. (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir Nelfinavirincreases the effect and toxicity of amiodarone (source: Drug Bank)
nelfinavir Nelfinavirincreases the effect and toxicity of amiodarone (source: Drug Bank)
nelfinavir This CYP3A4 inhibitor increases the effect and toxicity of aprepitant (source: Drug Bank)
nelfinavir Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
nelfinavir Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
nelfinavir Nelfinavir increases the effect and toxicity of the statin (source: Drug Bank)
nelfinavir Nelfinavir increases the effect and toxicity of the statin (source: Drug Bank)
nelfinavir Nelfinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if nelfinavir is initiated, discontinued or dose changed. Dosage adjustments may be required. (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir Increased effects/toxicity of ciclesonide (source: Drug Bank)
nelfinavir Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
nelfinavir Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of cyclosporine (source: Drug Bank)
nelfinavir The protease inhibitor, nelfinavir, may increase the effect of cyclosporine. (source: Drug Bank)
nelfinavir Nelfinavir may increase the serum concentration of dantrolene by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of dantrolene if nelfinavir is initiated, discontinued or dose changed. (source: Drug Bank)
nelfinavir This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolism (source: Drug Bank)
nelfinavir This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolism (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir Nelfinavir increases the effect and toxicity of ergot derivative (source: Drug Bank)
nelfinavir Nelfinavir increases the effect and toxicity of ergot derivative (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect and toxicity of eletriptan (source: Drug Bank)
nelfinavir The protease inhibitor, nelfinavir, may increase the effect and toxicity of eletriptan. (source: Drug Bank)
nelfinavir This protease inhibitor, nelfinavir, may increase the effect and toxicity of eplerenone. (source: Drug Bank)
nelfinavir Nelfinavir increases the effect and toxicity of ergot derivative (source: Drug Bank)
nelfinavir Nelfinavir increases the effect and toxicity of ergot derivative (source: Drug Bank)
nelfinavir This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
nelfinavir This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir Ritonavir could decrease the contraceptive efficacy (source: Drug Bank)
nelfinavir Ritonavir could decrease the contraceptive efficacy (source: Drug Bank)
nelfinavir Nelfinavir increases the effect and toxicity of felodipine (source: Drug Bank)
nelfinavir Nelfinavir increases the effect and toxicity of felodipine (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect and toxicity of fentanyl (source: Drug Bank)
nelfinavir The protease inhibitor, nelfinavir, may increase the effect and toxicity of fentanyl. (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir The protease inhibitor, nelfinavir, may increase the effect and toxicity of fusidic acid. (source: Drug Bank)
nelfinavir Nelfinavir increases the effect and toxicity of the statin (source: Drug Bank)
nelfinavir Nelfinavir increases the effect and toxicity of the statin (source: Drug Bank)
nelfinavir Nelfinavir decreases the effect of methadone (source: Drug Bank)
nelfinavir Nelfinavir decreases the effect of methadone (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of benzodiazepine (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of benzodiazepine (source: Drug Bank)
acenocoumarol The protease inhibitor increases the anticoagulant effect (source: Drug Bank)
acenocoumarol The protease inhibitor, nelfinavir, may increase the anticoagulant effect of acenocoumarol. (source: Drug Bank)
alprazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
alprazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
amiodarone Nelfinavir increases the effect and toxicity of amiodarone (source: Drug Bank)
amiodarone Nelfinavir increases the effect and toxicity of amiodarone (source: Drug Bank)
anisindione The protease inhibitor, nelfinavir, may increase the anticoagulant effect of anisindione. (source: Drug Bank)
aprepitant This CYP3A4 inhibitor increases the effect and toxicity of aprepitant (source: Drug Bank)
astemizole Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
astemizole Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
atorvastatin Nelfinavir increases the effect and toxicity of the statin (source: Drug Bank)
atorvastatin Nelfinavir increases the effect and toxicity of the statin (source: Drug Bank)
chlordiazepoxide The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
chlordiazepoxide The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
ciclesonide Increased effects/toxicity of ciclesonide (source: Drug Bank)
cisapride Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
cisapride Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
clonazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
clonazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
clorazepate The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
cyclosporine The protease inhibitor increases the effect of cyclosporine (source: Drug Bank)
cyclosporine The protease inhibitor, nelfinavir, may increase the effect of cyclosporine. (source: Drug Bank)
darifenacin This potent CYP3A4 inhibitor slows darifenacin / solifenacin metabolism (source: Drug Bank)
diazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
diazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
dicumarol The protease inhibitor increases the anticoagulant effect (source: Drug Bank)
dicumarol The protease inhibitor, nelfinavir, may increase the anticoagulant effect of dicumarol. (source: Drug Bank)
dihydroergotamine Nelfinavir increases the effect and toxicity of ergot derivative (source: Drug Bank)
eletriptan The protease inhibitor increases the effect and toxicity of eletriptan (source: Drug Bank)
eletriptan The protease inhibitor, nelfinavir, may increase the effect and toxicity of eletriptan. (source: Drug Bank)
eplerenone The protease inhibitor, nelfinavir, may increase the effect and toxicity of eplerenone. (source: Drug Bank)
ergotamine Nelfinavir increases the effect and toxicity of ergot derivative (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
estazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
estazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
ethinyl estradiol Ritonavir could decrease the contraceptive efficacy (source: Drug Bank)
felodipine Nelfinavir increases the effect and toxicity of felodipine (source: Drug Bank)
felodipine Nelfinavir increases the effect and toxicity of felodipine (source: Drug Bank)
fentanyl The protease inhibitor increases the effect and toxicity of fentanyl (source: Drug Bank)
fentanyl The protease inhibitor, nelfinavir, may increase the effect and toxicity of fentanyl. (source: Drug Bank)
flurazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
flurazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
halazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
lovastatin Nelfinavir increases the effect and toxicity of the statin (source: Drug Bank)
lovastatin Nelfinavir increases the effect and toxicity of the statin (source: Drug Bank)
mestranol Ritonavir could decrease the contraceptive efficacy (source: Drug Bank)
mestranol Ritonavir could decrease the contraceptive efficacy (source: Drug Bank)
methadone Nelfinavir decreases the effect of methadone (source: Drug Bank)
methadone Nelfinavir decreases the effect of methadone (source: Drug Bank)
midazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
midazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nevirapine Nevirapine decreases the effect of nelfinavir (source: Drug Bank)
nevirapine Nevirapine decreases the effect of nelfinavir (source: Drug Bank)
pimozide Nelfinavir increases the effect and toxicity of pimozide (source: Drug Bank)
pimozide Nelfinavir increases the effect and toxicity of pimozide (source: Drug Bank)
prazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
quazepam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
quinidine Nelfinavir increases the effect and toxicity of quinidine (source: Drug Bank)
quinidine Nelfinavir increases the effect and toxicity of quinidine (source: Drug Bank)
ranolazine Increased levels of ranolazine - risk of toxicity (source: Drug Bank)
rifampin Rifampin decreases the effect of nelfinavir (source: Drug Bank)
rifampin Rifampin decreases the effect of nelfinavir (source: Drug Bank)
sildenafil The protease inhibitor increases the effect and toxicity of sildenafil (source: Drug Bank)
sildenafil The protease inhibitor, nelfinavir, may increase the effect and toxicity of sildenafil. (source: Drug Bank)
simvastatin Nelfinavir increases the effect and toxicity of the statin (source: Drug Bank)
simvastatin Nelfinavir increases the effect and toxicity of the statin (source: Drug Bank)
solifenacin This potent CYP3A4 inhibitor slows darifenacin / solifenacin metabolism (source: Drug Bank)
sunitinib Possible increase in sunitinib levels (source: Drug Bank)
sunitinib Possible increase in sunitinib levels (source: Drug Bank)
tacrolimus The protease inhibitor increases the effect and toxicity of tacrolimus (source: Drug Bank)
tacrolimus The protease inhibitor, nelfinavir, may increase the effect and toxicity of tacrolimus. (source: Drug Bank)
terfenadine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
terfenadine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
triazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
triazolam The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
vardenafil The protease inhibitor increases the effect and toxicity of vardenafil (source: Drug Bank)
vardenafil The protease inhibitor, nelfinavir, may increase the effect and toxicity of vardenafil. (source: Drug Bank)
warfarin The protease inhibitor increases the anticoagulant effect (source: Drug Bank)
warfarin The protease inhibitor, nelfinavir, may increase the anticoagulant effect of warfarin. (source: Drug Bank)
nelfinavir Decreases the effect of nelfinavir (source: Drug Bank)
nelfinavir Decreases the effect of nelfinavir (source: Drug Bank)
nelfinavir Nelfinavir increases the effect and toxicity of pimozide (source: Drug Bank)
nelfinavir Nelfinavir increases the effect and toxicity of pimozide (source: Drug Bank)
nelfinavir Nelfinavir increases the effect and toxicity of quinidine (source: Drug Bank)
nelfinavir Nelfinavir increases the effect and toxicity of quinidine (source: Drug Bank)
nelfinavir Increased levels of ranolazine - risk of toxicity (source: Drug Bank)
nelfinavir Rifampin decreases the effect of nelfinavir (source: Drug Bank)
nelfinavir Rifampin decreases the effect of nelfinavir (source: Drug Bank)
nelfinavir The protease inhibitor, Nelfinavir, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Nelfinavir therapy is initiated, discontinued or altered. (source: Drug Bank)
nelfinavir Nelfinavir may reduce the metabolism of Tadalafil. Concomitant therapy should be avoided if possible due to high risk of Tadalafil toxicity. (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)
nelfinavir Nelfinavir, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Nelfinavir is initiated, discontinued, or dose changed. (source: Drug Bank)
nelfinavir Nelfinavir, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Nelfinavir is initiated, discontinued, or dose changed. (source: Drug Bank)
nelfinavir Nelfinavir may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects. (source: Drug Bank)
nelfinavir Nelfinavir may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided. (source: Drug Bank)
nelfinavir The strong CYP3A4 inhibitor, Nelfinavir, may decrease the metabolism and clearance of Teniposide, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Teniposide if Nelfinavir is initiated, discontinued or dose changed. (source: Drug Bank)
nelfinavir Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
nelfinavir Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
nelfinavir The strong CYP3A4 inhibitor, Nelfinavir, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Nelfinavir is initiated, discontinued or dose changed. (source: Drug Bank)
nelfinavir Nelfinavir may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity. (source: Drug Bank)
nelfinavir Nelfinavir may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity. (source: Drug Bank)
nelfinavir The p-glycoprotein inhibitor, Nelfinavir, 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)
nelfinavir Nelfinavir may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance. (source: Drug Bank)
nelfinavir The protease inhibitor, Nelfinavir, may increase the efficacy/toxicity of Trazodone by inhibiting Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Nelfinavir is initiated, discontinued or dose changed. (source: Drug Bank)
nelfinavir The protease inhibitor, Nelfinavir, may increase the efficacy/toxicity of Trazodone by inhibiting Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Nelfinavir is initiated, discontinued or dose changed. (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank)
nelfinavir The strong CYP3A4 inhibitor, Nelfinavir, may decrease the metabolism and clearance of Trimipramine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Trimipramine if Nelfinavir is initiated, discontinued or dose changed. (source: Drug Bank)
nelfinavir Nelfinavir, a strong CYP3A4 inhibitor, may reduce the metabolism and clearance of Vardenafil. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Vardenafil. (source: Drug Bank)
nelfinavir Nelfinavir, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Venlafaxine, a CYP3A4 substrate. Monitor for changes in therapeutic/adverse effects of Venlafaxine if Nelfinavir is initiated, discontinued, or dose changed. (source: Drug Bank)
nelfinavir Nelfinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of Veramapil, a CYP3A4 substrate, by decreasing its metabolism and clearance. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Verapamil if Nelfinavir is initiated, discontinued or dose changed. (source: Drug Bank)
nelfinavir Nelfinavir, a strong CYP3A4 inhibitor, may decrease the metabolism of Vinblastine. Consider alternate therapy to avoid Vinblastine toxicity. Monitor for changes in the therapeutic/adverse effects of Vinblastine if Nelfinavir is initiated, discontinued or dose changed. (source: Drug Bank)
nelfinavir Nelfinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of Vincristine by decreasing its metabolism. Consider alternate therapy to avoid Vincristine toxicity. Monitor for changes in the therapeutic and adverse effects of Vincristine if Nelfinavir is initiated, discontinued or dose changed. (source: Drug Bank)
nelfinavir Nelfinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of Vinorelbine by decreasing its metabolism. Consider alternate therapy to avoid Vinorelbine toxicity. Monitor for changes in the therapeutic and adverse effects of Vinorelbine if Nelfinavir is initiated, discontinued or dose changed. (source: Drug Bank)
nelfinavir Nelfinavir may decrease the serum concentration of voriconazole likely by increasing its metabolism. Voriconazole may increase the serum concentration of nelfinavir by decreasing its metabolism. Consider alternate therapy or adjust doses and monitor for reduced voriconazole efficacy and increased nelfinavir adverse effects during concomitant therapy. (source: Drug Bank)
nelfinavir Nelfinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if nelfinavir is initiated, discontinued or dose changed. (source: Drug Bank)
nelfinavir Nelfinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if nelfinavir is initiated, discontinued or dose changed. (source: Drug Bank)
nelfinavir Nelfinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zopiclone by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zopiclone if nelfinavir is initiated, discontinued or dose changed. (source: Drug Bank)

Curated Information ?

EvidenceDisease
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HIV
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HIV Infections

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

May Treat
Contraindicated With

Publications related to nelfinavir: 43

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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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Complex drug interactions of the HIV protease inhibitors 3: effect of simultaneous or staggered dosing of digoxin and ritonavir, nelfinavir, rifampin, or bupropion. Drug metabolism and disposition: the biological fate of chemicals. 2012. Kirby Brian J, et al. PubMed
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PharmGKB summary: very important pharmacogene information for cytochrome P450, family 2, subfamily C, polypeptide 19. Pharmacogenetics and genomics. 2011. Scott Stuart A, et al. PubMed
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Complex Drug Interactions of HIV Protease Inhibitors 2: In Vivo Induction and In Vitro to In Vivo Correlation of Induction of Cytochrome P450 1A2, 2B6 and 2C9 by Ritonavir or Nelfinavir. Drug metabolism and disposition: the biological fate of chemicals. 2011. Kirby Brian J, et al. PubMed
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Complex Drug Interactions of HIV Protease Inhibitors 1: Inactivation, Induction and Inhibition of Cytochrome P450 3A by Ritonavir or Nelfinavir. Drug metabolism and disposition: the biological fate of chemicals. 2011. Kirby Brian J, 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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Nuclear receptor-mediated induction of CYP450 by antiretrovirals: functional consequences of NR1I2 (PXR) polymorphisms and differential prevalence in whites and sub-Saharan Africans. Journal of acquired immune deficiency syndromes (1999). 2010. Svärd Jenny, 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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Influence of host genetic factors on efavirenz plasma and intracellular pharmacokinetics in HIV-1-infected patients. Pharmacogenomics. 2010. Elens Laure, et al. PubMed
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Effect of CYP2B6, ABCB1, and CYP3A5 polymorphisms on efavirenz pharmacokinetics and treatment response: an AIDS Clinical Trials Group study. The Journal of infectious diseases. 2010. Ribaudo Heather J, 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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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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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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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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Several major antiepileptic drugs are substrates for human P-glycoprotein. Neuropharmacology. 2008. Luna-Tortós Carlos, 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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Pharmacokinetics and pharmacodynamics of efavirenz and nelfinavir in HIV-infected children participating in an area-under-the-curve controlled trial. Clinical pharmacology and therapeutics. 2008. Fletcher C V, 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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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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Orosomucoid (alpha1-acid glycoprotein) plasma concentration and genetic variants: effects on human immunodeficiency virus protease inhibitor clearance and cellular accumulation. Clinical pharmacology and therapeutics. 2006. Colombo Sara, et al. PubMed
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Drug transporter and metabolizing enzyme gene variants and nonnucleoside reverse-transcriptase inhibitor hepatotoxicity. Clinical infectious diseases : an official publication of the Infectious Diseases Society of America. 2006. Ritchie Marylyn D, et al. PubMed
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Are plasma levels valid surrogates for cellular concentrations of antiretroviral drugs in HIV-infected patients?. Therapeutic drug monitoring. 2006. Colombo Sara, 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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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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Pharmacogenetics of long-term responses to antiretroviral regimens containing Efavirenz and/or Nelfinavir: an Adult Aids Clinical Trials Group Study. The Journal of infectious diseases. 2005. Haas David W, et al. PubMed
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Overview of the pharmacogenetics of HIV therapy. The pharmacogenomics journal. 2006. Rodríguez-Nóvoa S, et al. PubMed
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In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin glucuronidation. Drug metabolism and disposition: the biological fate of chemicals. 2005. Zhang Donglu, et al. PubMed
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Influence of single-nucleotide polymorphisms in the multidrug resistance-1 gene on the cellular export of nelfinavir and its clinical implication for highly active antiretroviral therapy. Antiviral therapy. 2004. Zhu Dayong, et al. PubMed
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Influence of lipid lowering fibrates on P-glycoprotein activity in vitro. Biochemical pharmacology. 2004. Ehrhardt Manuela, et al. PubMed
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Interactions of human P-glycoprotein with simvastatin, simvastatin acid, and atorvastatin. Pharmaceutical research. 2004. Hochman Jerome H, et al. PubMed
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Polymorphisms in human MDR1 (P-glycoprotein): recent advances and clinical relevance. Clinical pharmacology and therapeutics. 2004. Marzolini Catia, et al. PubMed
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Genetic polymorphisms of the human MDR1 drug transporter. Annual review of pharmacology and toxicology. 2003. Schwab Matthias, et al. PubMed
Response to antiretroviral treatment in HIV-1-infected individuals with allelic variants of the multidrug resistance transporter 1: a pharmacogenetics study. Lancet. 2002. Fellay Jacques, et al. PubMed
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Interaction of omeprazole, lansoprazole and pantoprazole with P-glycoprotein. Naunyn-Schmiedeberg's archives of pharmacology. 2001. Pauli-Magnus C, et al. PubMed
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The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. The Journal of clinical investigation. 1999. Greiner B, et al. PubMed
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Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Annual review of pharmacology and toxicology. 1999. Ambudkar S V, et al. PubMed
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Characterization of the selectivity and mechanism of human cytochrome P450 inhibition by the human immunodeficiency virus-protease inhibitor nelfinavir mesylate. Drug metabolism and disposition: the biological fate of chemicals. 1998. Lillibridge J H, et al. PubMed
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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
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P-glycoprotein structure and evolutionary homologies. Cytotechnology. 1993. Croop J M. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
63010-010-30
DrugBank:
DB00220
KEGG Compound:
C07257
PubChem Compound:
64143
PubChem Substance:
206971
46507719
Drugs Product Database (DPD):
2248761
BindingDB:
518
ChemSpider:
57718
Therapeutic Targets Database:
DAP000705
FDA Drug Label at DailyMed:
e72c2bc6-9462-4a2e-8e1d-b97592376cbd

Clinical Trials

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

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