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QuickView for tenofovir (compound)

Name: tenofovir
PubChem Compound ID: 122767
Molecular formula: C9H14N5O4P
Molecular weight: 287.213 g/mol
AIDS-042817; Phosphonic acid, (((1S)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy)methyl)-; (S)-PMPA; 147127-19-3; AIDS042817; (S)-9-(2-Phosphonylmethoxypropyl)adenine; Phosphonic acid, [[(1S)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]-
Name: tenofovir
Name (isomeric): DB00300
Drug Type: small molecule
Tenofovir disoproxil; D,L-Tenofovir; TDF; PMPA; Tenofovir disoproxil fumarate
Brand: Viread, Apropovir
Brand name mixture: Truvada(tenofovir + emtricitabine), Atripla(tenofovir + emtricitabine + efavirenz)
Category: Anti-HIV Agents, Nucleoside and Nucleotide Reverse Transcriptase Inhibitors, Reverse Transcriptase Inhibitors
CAS number: 147127-20-6
Indication: For use, in combination with other antiretroviral agents, for the treatment of HIV-1 infection.
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 acycl...
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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...
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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%.
Protein binding: Very low: < 0.7% to human plasma proteins and < 7.2% to serum proteins
Biotransformation: Neither tenofovir disoproxil nor tenofovir are substrates of CYP450 enzymes.
Half Life: Approximately 17 hours.
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.
Affected organisms: Human Immunodeficiency Virus
Drug interaction:
AtazanavirConcomitant 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.
DidanosineTenofovir may decrease the therapeutic effects and increase the adverse effects of Didanosine. Monitor for changes in virologic response and Didanosine toxicity during concomitant therapy.
ValganciclovirThe 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.