Bictegravir Sodium/Emtricitabine/Tenofovir Alafenamide Fumarate

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable fixed combination of bictegravir sodium, the sodium salt form of the human immunodeficiency virus type 1 (HIV-1) integrase strand transfer inhibitor (INSTI) bictegravir, emtricitabine, a nucleoside reverse transcriptase (RT) inhibitor (NRTI) analog of cytidine, and tenofovir alafenamide fumarate, the fumarate salt form of the lipophilic phosphonamidate prodrug of tenofovir, a NRTI analog of adenosine monophosphate, that is used to treat human immunodeficiency virus (HIV) infection. Upon oral administration of bictegravir/emtricitabine/tenofovir alafenamide, bictegravir inhibits the strand transfer activity of HIV-1 integrase, an HIV-1 coded enzyme that is necessary for viral replication. Inhibition of integrase prevents the integration of linear HIV-1 DNA into host genomic DNA. Emtricitabine and tenofovir inhibit the activity of HIV RT by competing with natural deoxyribonucleosides for incorporation into the growing viral DNA chain resulting in early chain termination. This interferes with the generation of DNA copies of viral RNA, which is necessary for the synthesis of new virions.

**Synonyms:** - Biktarvy - Biktarvy