Drug/Small Molecule:
tenofovir

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

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.

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

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

PGx Test Variants Assayed Gene?

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

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

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

Gene ? Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No VIP available VA ABCC10 H1 N/A N/A N/A
No VIP available No VIP available VA ABCC2 H2 N/A N/A N/A
No VIP available No Clinical Annotations available 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
rs11231809 64302950T>A, 9608745T>A
T > A
Not Available
No VIP available No Clinical Annotations available VA
rs1128503 1236T>C, 167964T>C, 25043506A>G, 87550285A>G, ABCB1 1236C>T, ABCB1*8, ABCB1: c.1236T>C, ABCB1:1236C>T, ABCB1:1236T>C, Gly412=, Gly412Gly, mRNA 1654T>C, p.Gly412Gly
A > G
Not Available
Gly412Gly
No VIP available No Clinical Annotations available VA
rs11568626 149G>A, 62752014C>T, 8057809C>T, Arg50His
C > T
Missense
Arg50His
No VIP available No Clinical Annotations available VA
rs11568655 3310T>C, 8804690A>G, 95715014A>G, Leu1104=
A > G
Synonymous
Leu1104Leu
No VIP available No Clinical Annotations available VA
rs11568658 559G>T, 8952684C>A, 95863008C>A, ABCC4 : G187W, Gly187Trp
C > A
Missense
Gly187Trp
No VIP available No Clinical Annotations available VA
rs11568695 3609G>A, 8786216C>T, 95696540C>T, Ala1203=
C > T
Synonymous
Ala1203Ala
No VIP available No Clinical Annotations available VA
rs1557070 1497C>T, 8928679G>A, 95839003G>A, Tyr499=
G > A
Synonymous
Tyr499Tyr
No VIP available CA VA
rs17222723 101595996T>A, 3563T>A, 52400460T>A, 58534T>A, ABCC2 rs8187694, MRP2 Val1188Glu, Val1188Glu
T > A
Missense
Val1188Glu
No VIP available CA VA
rs1751034 3348G>A, 8804652C>T, 95714976C>T, ABCC4: 3463 A>G, Lys1116=
C > T
Synonymous
Lys1116Lys
No VIP available No Clinical Annotations available VA
rs2125739 2759T>C, 2843T>C, 43352865T>C, 43412865T>C, Ile920Thr, Ile948Thr
T > C
Missense
Ile948Thr
No VIP available CA 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
rs2274405 8948654T>C, 95858978T>C, 969A>G, Ser323=
T > C
Synonymous
Ser323Ser
No VIP available No Clinical Annotations available VA
rs2274406 8948672T>C, 951A>G, 95858996T>C, Arg317=
T > C
Synonymous
Arg317Arg
No VIP available No Clinical Annotations available VA
rs2274407 8948711C>A, 8948711C>G, 8948711C>T, 912G>A, 912G>C, 912G>T, 95859035C>A, 95859035C>G, 95859035C>T, Lys304=, Lys304Asn
C > G
C > T
C > A
Missense
Lys304Lys
Lys304Asn
No VIP available No Clinical Annotations available VA
rs3740066 101604207C>T, 3972C>T, 52408671C>T, 66745C>T, ABCC2:3972C>T, I1324I, Ile1324=
C > T
Synonymous
Ile1324Ile
No VIP available No Clinical Annotations available VA
rs3742106 *38T>G, 8763467A>C, 95673791A>C
A > C
3' UTR
No VIP available No Clinical Annotations available VA
rs7080681 101560169G>A, 1058G>A, 22707G>A, 52364633G>A, Arg353His
G > A
Missense
Arg353His
No VIP available CA VA
rs717620 -24C>T, 101542578C>T, 5116C>T, 52347042C>T, ABCC2: 5'UTR, ABCC2:(-24)C>T, mRNA 118C>T
C > T
5' UTR
No VIP available No Clinical Annotations available VA
rs8187710 101611294G>A, 4544G>A, 52415758G>A, 73832G>A, ABCC2 rs8187710, Cys1515Tyr, MRP2 Cys1515Tyr
G > A
Missense
Cys1515Tyr
No VIP available No Clinical Annotations available VA
rs899494 669T>C, 8951480A>G, 95861804A>G, Ile223=
A > G
Synonymous
Ile223Ile
No VIP available CA VA
rs9349256 1791+526G>A, 1875+526G>A, 43344511G>A, 43404511G>A
G > A
Intronic
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • D,L-Tenofovir
  • PMPA
  • TDF
  • Tenofovir disoproxil
  • Tenofovir disoproxil fumarate
Trade Names
  • Apropovir
  • Viread
Brand Mixture Names
  • Atripla (tenofovir + emtricitabine + efavirenz)
  • Truvada (tenofovir + emtricitabine)

PharmGKB Accession Id:
PA10204

Description

Tenofovir, marketed by Gilead Sciences under the trade name Viread R , belongs to a class of antiretroviral drugs known as nucleotide analogue reverse transcriptase inhibitors (nRTIs), which block reverse transcriptase, an enzyme crucial to viral production in HIV-infected people. Wikipedia

Source: Drug Bank

Indication

For use, in combination with other antiretroviral agents, for the treatment of HIV-1 infection.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Tenofovir inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5'-triphosphate and, after incorporation into DNA, by DNA chain termination. Specifically, the drugs are analogues of the naturally occurring deoxynucleotides needed to synthesize the viral DNA and they compete with the natural deoxynucleotides for incorporation into the growing viral DNA chain. However, unlike the natural deoxynucleotides substrates, NRTIs and NtRTIs (nucleoside/tide reverse transcriptase inhibitors) lack a 3'-hydroxyl group on the deoxyribose moiety. As a result, following incorporation of an NRTI or an NtRTI, the next incoming deoxynucleotide cannot form the next 5'-3' phosphodiester bond needed to extend the DNA chain. Thus, when an NRTI or NtRTI is incorporated, viral DNA synthesis is halted, a process known as chain termination. All NRTIs and NtRTIs are classified as competitive substrate inhibitors.

Source: Drug Bank

Pharmacology

Tenofovir belongs to a class of antiretroviral drugs known as nucleotide analogue reverse transcriptase inhibitors (NtRTIs), which block reverse transcriptase, an enzyme crucial to viral production in HIV-infected people. Tenofovir is currently in late-stage clinical trials for the treatment of hepatitis B. Tenofovir disoproxil fumarate is an acyclic nucleoside phosphonate diester analog of adenosine monophosphate. Tenofovir requires initial diester hydrolysis for conversion to tenofovir and subsequent phosphorylations by cellular enzymes to form tenofovir diphosphate. Tenofovir diphosphate is a weak inhibitor of mammalian DNA polymerases alpha, beta, and mitochondrial DNA polymerase gamma.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Neither tenofovir disoproxil nor tenofovir are substrates of CYP450 enzymes.

Source: Drug Bank

Protein Binding

Very low: < 0.7% to human plasma proteins and < 7.2% to serum proteins

Source: Drug Bank

Absorption

The oral bioavailability in fasted patients is approximately 25%. Administration of food (high fat meal containing 40 to 50% fat) increases the oral bioavailability, with an increase in the AUC of approximately 40%.

Source: Drug Bank

Half-Life

Approximately 17 hours.

Source: Drug Bank

Toxicity

Limited clinical experience at doses higher than the therapeutic dose of tenofovir 300 mg is available. In Study 901 tenofovir disoproxil fumarate 600 mg was administered to 8 patients orally for 28 days. No severe adverse reactions were reported. The effects of higher doses are not known.

Source: Drug Bank

Volume of Distribution

Source: Drug Bank

Chemical Properties

Chemical Formula

C9H14N5O4P

Source: Drug Bank

Isomeric SMILES

C[C@H](CN1C=NC2=C(N=CN=C21)N)OCP(=O)(O)O

Source: Drug Bank

C[C@H](CN1C=NC2=C1N=CN=C2N)OCP(O)(O)=O

Source: Drug Bank

Canonical SMILES

C[C@H](CN1C=NC2=C1N=CN=C2N)OCP(O)(O)=O

Source: Drug Bank

Average Molecular Weight

287.2123

Source: Drug Bank

Monoisotopic Molecular Weight

287.078340473

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Tenofovir/Adefovir Pathway, Pharmacokinetics
    Representation of candidate genes involved in renal elimination of tenofovir and adefovir and their mechanism of action in an infected kidney cell

External Pathways

Links to non-PharmGKB pathways.

PharmGKB contains no links to external pathways for this drug. To report a pathway, click here.

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
tenofovir Tenofovir decreases the levels/effects of atazanavir (source: Drug Bank)
tenofovir Tenofovir decreases the levels/effects of atazanavir (source: Drug Bank)
tenofovir Tenofovir increases the effect and toxicity of didanosine (source: Drug Bank)
tenofovir Tenofovir increases the effect and toxicity of didanosine (source: Drug Bank)
atazanavir Tenofovir decreases the levels/effects of atazanavir (source: Drug Bank)
atazanavir Concomitant therapy may result in decreased serum levels of Atazanavir and increased levels of Tenofovir. Concomitant therapy should only be used with the inclusion of Ritonavir. (source: Drug Bank)
didanosine Tenofovir increases the effect and toxicity of didanosine (source: Drug Bank)
didanosine Tenofovir may decrease the therapeutic effects and increase the adverse effects of Didanosine. Monitor for changes in virologic response and Didanosine toxicity during concomitant therapy. (source: Drug Bank)
tenofovir The excretion rates of Valganciclovir and/or Tenofovir may decrease as both drugs are eliminated by active tubular secretion. Monitor for increased serum concentrations and toxicity of both agents. (source: Drug Bank)
tenofovir The excretion rates of Valganciclovir and/or Tenofovir may decrease as both drugs are eliminated by active tubular secretion. Monitor for increased serum concentrations and toxicity of both agents. (source: Drug Bank)

Curated Information ?

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

May Treat
Contraindicated With

Publications related to tenofovir: 12

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Mitochondrial DNA Variation and Changes in Adiponectin and Endothelial Function in HIV-Infected Adults After Antiretroviral Therapy Initiation. AIDS research and human retroviruses. 2013. Hulgan Todd, 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
Potential effect of pharmacogenetics on maternal, fetal and infant antiretroviral drug exposure during pregnancy and breastfeeding. Pharmacogenomics. 2012. Olagunju Adeniyi, 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
The Dual Role of Pharmacogenetics in HIV Treatment: Mutations and Polymorphisms Regulating Antiretroviral Drug Resistance and Disposition. Pharmacological reviews. 2012. Michaud Veronique, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Genetic variants of ABCC10, a novel tenofovir transporter, are associated with kidney tubular dysfunction. The Journal of infectious diseases. 2011. Pushpakom Sudeep 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
Pharmacogenomics of membrane transporters: past, present and future. Pharmacogenomics. 2010. Yee Sook Wah, 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 of tenofovir treatment. Pharmacogenomics. 2009. Rodriguez-Novoa Sonia, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Predictors of kidney tubular dysfunction in HIV-infected patients treated with tenofovir: a pharmacogenetic study. Clinical infectious diseases : an official publication of the Infectious Diseases Society of America. 2009. Rodríguez-Nóvoa Sonia, 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
Population pharmacokinetics of tenofovir in HIV-1-infected pregnant women and their neonates (ANRS 12109). Clinical pharmacology and therapeutics. 2009. Hirt D, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Clinical and genetic determinants of intracellular tenofovir diphosphate concentrations in HIV-infected patients. Journal of acquired immune deficiency syndromes (1999). 2008. Kiser Jennifer J, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
The effect of lopinavir/ritonavir on the renal clearance of tenofovir in HIV-infected patients. Clinical pharmacology and therapeutics. 2008. Kiser J J, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Association between ABCC2 gene haplotypes and tenofovir-induced proximal tubulopathy. The Journal of infectious diseases. 2006. Izzedine Hassane, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Functional consequences of single nucleotide polymorphisms in the human organic anion transporter hOAT1 (SLC22A6). The Journal of pharmacology and experimental therapeutics. 2005. Bleasby Kelly, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
53808-0810-1
DrugBank:
DB00300
PDB:
TFO
KEGG Drug:
D01982
PubChem Compound:
464205
PubChem Substance:
46508131
699321
Drugs Product Database (DPD):
2247128
ChemSpider:
408154
HET:
TFO
Therapeutic Targets Database:
DAP001430
FDA Drug Label at DailyMed:
e122435e-cd0b-4c90-940a-b7a0d090d866

Clinical Trials

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

Common Searches

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