Tenofovir alafenamide, sold under the brand name Vemlidy, is a hepatitis B virus (HBV) nucleotide reverse transcriptase inhibitor medication for the treatment of chronic hepatitis B virus (HBV) infection in adults with compensated liver disease. It is taken by mouth. Tenofovir alafenamide is a

prodrug A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug ...

of tenofovir. It was developed by Gilead Sciences based on the protide technology of Chris McGuigan for use in the treatment of HIV/AIDS and chronic hepatitis B, and is applied in the form of tenofovir alafenamide

fumarate Fumaric acid is an organic compound with the formula HO2CCH=CHCO2H. A white solid, fumaric acid occurs widely in nature. It has a fruit-like taste and has been used as a food additive. Its E number is E297. The salts and esters are known as f ...

(TAF). Closely related to the commonly used reverse-transcriptase inhibitor

tenofovir disoproxil fumarate Tenofovir disoproxil, sold under the trade name Viread among others, is a medication used to treat chronic hepatitis B and to prevent and treat HIV/AIDS. It is generally recommended for use with other antiretrovirals. It may be used for preven ...

(TDF), TAF has greater antiviral activity and better distribution into lymphoid tissues than that agent. Vemlidy was approved by the U.S. Food and Drug Administration (FDA) in November 2016.

Fixed-dose combinations containing tenofovir alafenamide

* Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide (Genvoya) — approved both in the United States and in the European Union in November 2015 (compare elvitegravir/cobicistat/emtricitabine/tenofovir; (Stribild)) * Emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey) — approved in the United States in March 2016, and in the European Union in June 2016 (compare

Emtricitabine/rilpivirine/tenofovir Emtricitabine/rilpivirine/tenofovir (trade names Complera, Eviplera) is a fixed-dose combination of antiretroviral drugs for the treatment of HIV/AIDS. The drug was co-developed by Gilead Sciences and Johnson & Johnson's Tibotec division and w ...

; (Complera)) * Emtricitabine/tenofovir alafenamide (Descovy) — approved in the United States in April 2016 (compare emtricitabine/tenofovir; (Truvada)). In October 2019, Descovy was approved in the United States for HIV-1 pre-exposure prophylaxis (PrEP). * Bictegravir/emtricitabine/tenofovir alafenamide (Biktarvy) — approved in the United States in February 2018. * Darunavir/cobicistat/emtricitabine/tenofovir alafenamide (Symtuza) — approved in the European Union in September 2017, in the United States in July 2018, and in Australia in November 2019. * Dolutegravir/emtricitabine/tenofovir alafenamide. * Dolutegravir/lamivudine/tenofovir alafenamide.

Research

Gilead announced a Phase III clinical trial evaluating a single-tablet regimen combining tenofovir alafenamide with cobicistat, emtricitabine and elvitegravir and developed a coformulation of the drug with cobicistat, emtricitabine and the protease inhibitor darunavir. In a 48-week study comparing elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil (Stribild) to elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide (Genvoya), the results showed the newer drug's effects 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.Horn, T. et al
Tenefovir Alafenamide Fumarate (TAF) Sign-On Letter to Gilead
. 13 June 2013. Treatment Action Group. The FDA approved the TAF-based treatment regimen for treatment of HIV-1 in November 2015. Genvoya is the first TAF-based regimen to receive approval.

References

External links

* * {{DEFAULTSORT:Tenofovir Alafenamide Carboxylate esters Fixed dose combination (antiretroviral) Gilead Sciences Isopropyl esters Nucleoside analog reverse transcriptase inhibitors Organophosphates Phenol esters Pre-exposure prophylaxis