Tenofovir

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Tenofovir
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200px
Systematic (IUPAC) name
({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)phosphonic acid
Clinical data
Pregnancy
category
Routes of
administration		 Oral
Legal status
Legal status
  • ℞-only (U.S.), POM (UK)
Pharmacokinetic data
Bioavailability 25%
Protein binding < 1%
Biological half-life 17 hours
Excretion Renal
Identifiers
CAS Number 147127-20-6
ATC code J05AF07 (WHO)
PubChem CID 464205
DrugBank APRD01248
Chemical data
Formula C9H14N5O4P
Molar mass 287.213 g/mol[[Script error: No such module "String".]]
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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 (nRTIs), which block reverse transcriptase, an enzyme crucial to viral production in HIV-infected people.

Drug forms

Tenofovir disoproxil fumarate is a prodrug form of Tenofovir. 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 daily dose for the treatment of HIV.

History

Tenofovir was discovered through a collaborative research effort between Antonín Holý at the Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic (IOCB) in Prague, and 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 for the treatment of HIV, and on August 11, 2008 for the treatment of chronic hepatitis B[2][3].

Indications

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 the clinical progression of HIV. It also has activity against wild-type and lamivudine-resistant HBV.

Adverse effects and drug interactions

The most common side effects associated with tenofovir include nausea, vomiting, diarrhea, and asthenia. Less frequent side effects include hepatotoxicity, abdominal pain, and flatulence.[4] Tenofovir has also been implicated in causing renal toxicity, particularly at elevated concentrations.[5]

Tenofovir can cause acute renal failure, Fanconi syndrome, proteinuria or tubular necrosis. These side effects are due to accumulation of the drug in proximal tubules. Tenofovir can interact with didanosine by increasing didanosine's concentration. It also decreases the concentration of atazanavir sulfate.

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 the 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.[6] [7] In July 2010, a vaginal gel containing tenofovir, a reverse transcriptase inhibitor, was shown to reduce HIV infection rates by 39 percent in a trial conducted in South Africa.[8]

External links

References

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Antiviral drugs: antiretroviral drugs used against HIV (primarily J05)
Entry/fusion inhibitors
(Discovery & development)
Reverse transcriptase
inhibitors (RTIs)
(1st gen) Efavirenz°# · Nevirapine#  · Loviride◊ · Delavirdine◊ ·
(2nd gen) diarylpyrimidines (Etravirine, Rilpivirine†)  · Lersivirine†
Integrase inhibitors
Raltegravir · Elvitegravir† · Globoidnan A (experimental)  · MK-2048†  · GSK-572†
Maturation inhibitors
Bevirimat† · Vivecon†
Protease Inhibitors (PI)
(Discovery and development)
Combined formulations
Experimental agents
TRIM5alpha (gene)
Other
Failed agents
°DHHS preferred first-line agent. ◊Formerly or rarely used agent.
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  1. ↑ Emau P, Jiang Y, Agy MB; et al. (2006). "Post-exposure prophylaxis for SIV revisited: Animal model for HIV infection". AIDS Res Ther. 3: 29. doi:10.1186/1742-6405-3-29. PMC 1687192 Freely accessible. PMID 17132170. 
  2. ↑ FDA letter of approval (regarding treatment of hepatitis B)
  3. ↑ FDA Clears Viread for Hepatitis B
  4. ↑ USPDI. Thompson. 2005. pp. 2741–2. 
  5. ↑ "Viread Prescribing Guidelines" (PDF). U.S. Food and Drug Administration. March 2006. Retrieved 2007-02-12. 
  6. ↑ "Tenofovir Use Safe for Uninfected, West African Women at Risk of HIV Infection". Family Health International. 2006-08-17. Retrieved 2007-06-01. 
  7. ↑ "Additional Studies Needed to Assess Effectiveness of Tenofovir for Prevention". Family Health International. Retrieved 2007-06-01. 
  8. ↑ Karim, Q. A., Karim, S. S. A., Frolich, J. A., Grobler, A. C., Baxter, C., Mansoor, L. E., Kharsany, A. B. M., Sibeko, S., Mlisana, K. P., Omar, Z., Gengiah, T. N., Maarschalk, S., Arulappan, N., Mlotshwa, M., Morris, L., and Taylor, D. (19 July 2010). "Effectiveness and Safety of Tenofovir Gel, an Antiretroviral Microbicide, for the Prevention of HIV Infection in Women". Science. 329 (5996): 1168–74. doi:10.1126/science.1193748. PMID 20643915. 
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