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Tenofovir alafenamide
Tenofovir alafenamide (INN/USAN, formerly GS-7340) is a nucleotide reverse transcriptase inhibitor and a prodrug of tenofovir. It is under development by Gilead Sciences for use in the treatment of HIV infection and chronic hepatitis B, and is applied in the form of tenofovir alafenamide fumarate (TAF). Closely related to the commonly used reverse-transcriptase inhibitor tenofovir disoproxil, TAF has greater antiviral activity and better distribution into lymphoid tissues than that agent.〔M Markowitz, A Zolopa, et al. (GS-7340 Demonstrates Greater Declines in HIV-1 RNA than Tenofovir Disoproxil Fumarate During 14 Days of Monotherapy in HIV-1 Infected Subjects ). 18th Conference on Retroviruses and Opportunistic Infections 2 Mar 2011. Paper # 152LB〕
Gilead has announced a phase 3 clinical trial evaluating a single-tablet regimen combining tenofovir alafenamide with cobicistat, emtricitabine and elvitegravir and plans to coformulate the drug with cobicistat, emtricitabine and the protease inhibitor darunavir.〔(GS-7340 Packs Greater HIV Punch, Potentially Better Safety, Versus Viread ) Horn, Tim. 15 Mar 2012. AIDSmeds.com〕〔( Pharmacokinetics of a Novel EVG/COBI/FTC/GS-7340 Single Tablet Regimen ). 13th International Workshop on Clinical Pharmacology of HIV Therapy. Barcelona, Spain. April 16-18, 2012. 〕 In a 48 week study comparing elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil to elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide, the results showed the prodrug to be non inferior to the established agent, but at much lower dosages and with lower incidence of adverse side effects such as impaired kidney function.〔(Once-Daily Tenofovir Prodrug Combo Pill as Effective as Stribild ). AIDSmeds.com 1 Nov 2012.〕〔(CROI 2013: New Pro-drug Tenofovir Alafenamide Appears Equally Effective but Better Tolerated ). Highleyman, Liz. HIVandHepatitis.com. 6 March 2013.〕〔Horn, T. et al. (Tenefovir Alafenamide Fumarate (TAF) Sign-On Letter to Gilead ). 13 June 2013. Treatment Action Group. 〕
== See also ==
* Sofosbuvir — an antiviral drug bearing structural similarity (phosphoramidate side chain which is metabolised by cathepsin A, carboxylesterase 1 and histidine triad nucleotide-binding protein 1 (HINT1))〔(【引用サイトリンク】url=https://yixiblog.wordpress.com/tag/tenofovir-alafenamide-fumarate/ )〕
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