Tenofovir alafenamide, sold under the brand name Vemlidy, is a hepatitis B virus (HBV)

nucleotide Nucleotides are organic molecules consisting of a nucleoside and a phosphate. They serve as monomeric units of the nucleic acid polymers – deoxyribonucleic acid (DNA) and ribonucleic acid (RNA), both of which are essential biomolecules wi ...

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 The ProTide technology is a prodrug approach used in molecular biology and drug design. It is designed to deliver nucleotide analogues (as monophosphate) into the cell (ProTide: PROdrug + nucleoTIDE). It was invented by Professor Chris McGuigan (Sc ...

technology of Chris McGuigan for use in the treatment of

HIV/AIDS Human immunodeficiency virus infection and acquired immunodeficiency syndrome (HIV/AIDS) is a spectrum of conditions caused by infection with the human immunodeficiency virus (HIV), a retrovirus. Following initial infection an individual ...

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 The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respon ...

(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 Elvitegravir/cobicistat/emtricitabine/tenofovir, sold under the brand name Stribild, also known as the Quad pill, is a fixed-dose combination antiretroviral medication for the treatment of HIV/AIDS. Elvitegravir, emtricitabine and tenofovir diso ...

; (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; (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 Darunavir (DRV), sold under the brand name Prezista among others, is an antiretroviral medication used to treat and prevent HIV/AIDS. It is generally recommended for use with other antiretrovirals. It is often used with low doses of ritonavir or ...

. In a 48-week study comparing

elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil Elvitegravir/cobicistat/emtricitabine/tenofovir, sold under the brand name Stribild, also known as the Quad pill, is a fixed-dose combination antiretroviral medication for the treatment of HIV/AIDS. Elvitegravir, emtricitabine and tenofovir diso ...

(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