Article: Tenofovir

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Tenofovir
Systematic (IUPAC) name
1-(6-aminopurin-9-yl) propan-2-yloxymethylphosphonic acid
Identifiers
CAS number 147127-20-6
ATC code J05AF07
PubChem 464205
DrugBank APRD01248
Chemical data
Formula C9H14N5O4P 
Mol. weight 287.213 g/mol
Pharmacokinetic data
Bioavailability 25%
Protein binding < 1%
Metabolism  ?
Half life 17 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

B (U.S.)

Legal status

â„ž-only (U.S.), POM (UK)

Routes Oral
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Viread Logo
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Tenofovir disoproxil fumarate

Tenofovir disoproxil fumarate (TDF), marketed by Gilead Sciences under the trade name Viread®, 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 also available in a fixed-dose combination with emtricitabine in a product with the brand name Truvada® for once-a-day dosing. (Emtricitabine is marketed as a single-compound product called Emtriva®, also by Gilead.) A fixed-dose triple combination of tenofovir, emtricitabine and efavirenz (Sustiva®, marketed by Bristol-Myers Squibb) is in development.

Tenofovir is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults. This indication is based on analyses of plasma HIV-1 RNA levels and CD4 cell counts in controlled studies of tenofovir in treatment-naïve and treatment-experienced adults. There are no study results demonstrating the effect of tenofovir on clinical progression of HIV.

History

Tenofovir was discovered through a collaborative research effort between Dr Antonin Holy at the Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic (IOCB) in Prague, and Dr Erik DeClercq, Rega Institute for Medical Research, Catholic University of Leuven, Belgium.

Tenofovir was approved by the U.S. Food and Drug Administration (FDA) on October 26, 2001. It is currently in late-stage clinical trials for the treatment of hepatitis B.

The fixed-dose combination of tenofovir with emtricitabine was approved on August 2, 2004 for once-a-day dosing. The fixed-dose triple combination of tenofovir, emtricitabine and efavirenz is in development.

Resources

  • PMPA (Drug Digest)
  • TDF (Drug Digest)