Bictegravir/emtricitabine/tenofovir AF

HIV Infection

Once-daily single tablet regimen pending FDA approval for HIV infection that contains bictegravir (BIC) 50 mg, emtricitabine (FTC) 200 mg, and tenofovir alafenamide (TAF) 25 mg

Mechanism of Action

Bictegravir: HIV-1 integrase strand transfer inhibitor (INSTI); inhibits HIV-1 replication by blocking the strand transfer step of viral DNA integration into the host genome; novel INSTI since it can be dose once daily without boosting

Emtricitabine: Nucleoside reverse transcriptase inhibitor (NRTI); cytosine analog phosphorylated to emtricitabine 5'-triphosphate causing inhibition of HIV and RNA dependent DNA polymerase

Tenofovir alafenamide (AF): NRTI prodrug of tenofovir; compared with tenofovir disoproxil fumarate (tenofovir DF, Viread), tenofovir alafenamide (AF) is a more targeted form of tenofovir that has demonstrated high antiviral efficacy at a dose that is 10 times lower than tenofovir DF, as well as an improved renal and bone safety profile; inhibits HIV-1 RT by competing with the natural substrate deoxyadenosine 5′-triphosphate and, after incorporation into DNA, by DNA chain termination