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 Reverse-transcriptase inhibitors (RTIs) are a class of antiretroviral drugs used to treat HIV infection or AIDS, and in some cases hepatitis B. RTIs inhibit activity of reverse transcriptase, a viral DNA polymerase that is required for replicati ...

medication for the treatment of chronic hepatitis B virus (HBV) infection in adults with compensated liver disease. It is taken

by mouth Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are i ...

. 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 ...

tenofovir 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 ...

. It was developed by

Gilead Sciences Gilead Sciences, Inc. () is an American biopharmaceutical company headquartered in Foster City, California, that focuses on researching and developing antiviral drugs used in the treatment of HIV/AIDS, hepatitis B, hepatitis C, influenza, and CO ...

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 (S ...

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 Hepatitis B is an infectious disease caused by the ''Hepatitis B virus'' (HBV) that affects the liver; it is a type of viral hepatitis. It can cause both acute and chronic infection. Many people have no symptoms during an initial infection. Fo ...

, 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 tissue The lymphatic system, or lymphoid system, is an organ system in vertebrates that is part of the immune system, and complementary to the circulatory system. It consists of a large network of lymphatic vessels, lymph nodes, lymphatic or lymphoid o ...

s 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 Emtricitabine/tenofovir, sold under the brand name Truvada among others, is a fixed-dose combination antiretroviral medication used to treat and prevent HIV/AIDS. It contains the antiretroviral medications emtricitabine and tenofovir disopro ...

; (Truvada)). In October 2019, Descovy was approved in the United States for HIV-1

pre-exposure prophylaxis Pre-exposure prophylaxis (PrEP) is the use of medications to prevent the spread of disease in people who have not yet been exposed to a disease-causing agent, usually a virus. The term typically refers to the use of antiviral drugs as a strate ...

(PrEP). *

Bictegravir/emtricitabine/tenofovir alafenamide Bictegravir/emtricitabine/tenofovir alafenamide, sold under the brand name Biktarvy, is a fixed-dose combination antiretroviral medication for the treatment of HIV/AIDS. One tablet, taken orally once daily, contains 50mg bictegravir, 200mg emt ...

(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 Cobicistat, sold under the brand name Tybost, is a medication for use in the treatment of human immunodeficiency virus infection (HIV/AIDS). Its major mechanism of action is through the inhibition of human CYP3A proteins. Like ritonavir (Norv ...

emtricitabine Emtricitabine (commonly called FTC, systematic name 2',3'-dideoxy-5-fluoro-3'-thiacytidine), with trade name Emtriva (formerly Coviracil), is a nucleoside reverse-transcriptase inhibitor (NRTI) for the prevention and treatment of HIV infection i ...

and

elvitegravir Elvitegravir (EVG) is an integrase inhibitor used to treat HIV infection. It was developed by the pharmaceutical company Gilead Sciences, which licensed EVG from Japan Tobacco in March 2008. The drug gained approval by the U.S. Food and Drug ...

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