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	J05 AF07
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	℞-only (U.S.), POM (UK)
Routes	Oral

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Tenofovir disoproxil fumarate

Tenofovir disoproxil fumarate (TDF or PMPA^[1]), 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.) Atripla®, a fixed-dose triple combination of tenofovir, emtricitabine and efavirenz, was approved by the FDA on 12 July 2006 and is now available, providing a single dose once per day for treatment of HIV.

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.

[edit] History

Tenofovir was discovered through a collaborative research effort between Dr Antonín Holý 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.

[edit] HIV Risk Reduction

A 2006 trial by Family Health International gave either Viread or a placebo to 936 high-risk women in Cameroon, Ghana and Nigeria. While results show signs that the Viread group contracted HIV at a reduced rate, the researchers cautioned against drawing conclusions from the study because the sample size was so small.

[edit] External links

Antivirals (primarily J05A, also S01AD and D06BB) edit

Anti-herpesvirus agents		Aciclovir, Cidofovir, Docosanol, Famciclovir, Fomivirsen, Foscarnet, Ganciclovir, Idoxuridine, Penciclovir, Trifluridine, Tromantadine, Valaciclovir, Valganciclovir, Vidarabine
Anti-influenza agents		Amantadine, Oseltamivir, Peramivir, Rimantadine, Zanamivir

Antiretroviral drugs	NRTIs	Abacavir, Didanosine, Emtricitabine, Lamivudine, Stavudine, Zalcitabine, Zidovudine
	NtRTIs	Tenofovir
	NNRTIs	Efavirenz, Delavirdine, Nevirapine
	PIs	Amprenavir, Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir, Nelfinavir, Ritonavir, Saquinavir, Tipranavir
	Fusion inhibitors	Enfuvirtide

Other antiviral agents		Adefovir, Fomivirsen, Imiquimod, Inosine,Interferon, Podophyllotoxin, Ribavirin, Viramidine