Bictegravir/Emtricitabine/Tenofovir Alafenamide: A Review in HIV-1 Infection.
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Deeks ED
Bictegravir/Emtricitabine/Tenofovir Alafenamide: A Review in HIV-1 Infection.
Drugs. 2018 Nov;78(17):1817-1828. doi: 10.1007/s40265-018-1010-7.
- PubMed ID
- 30460547 [ View in PubMed]
- Abstract
Bictegravir is a new integrase strand transfer inhibitor (INSTI) with a high genetic barrier to the development of HIV-1 resistance. The drug is co-formulated with the nucleos(t)ide reverse transcriptase inhibitors emtricitabine and tenofovir alafenamide (AF) in a single-tablet regimen (STR) for the once-daily treatment of HIV-1 infection in adults (bictegravir/emtricitabine/tenofovir AF; Biktarvy((R))). In phase 3 trials, bictegravir/emtricitabine/tenofovir AF was noninferior to dolutegravir-based therapy (dolutegravir/abacavir/lamivudine or dolutegravir plus emtricitabine/tenofovir AF) in establishing virological suppression in treatment-naive adults through 96 weeks' treatment and, similarly, was noninferior to ongoing dolutegravir/abacavir/lamivudine or boosted elvitegravir- or protease inhibitor (PI)-based therapy in preventing virological rebound over 48 weeks in treatment-experienced patients. No resistance emerged to any of the antiretrovirals in the STR. Bictegravir/emtricitabine/tenofovir AF is generally well tolerated, requires no prior HLA-B*5701 testing (making it more suitable for 'rapid start' treatment), fulfils the antiretroviral regimen requirement for patients with hepatitis B virus (HBV) co-infection (i.e. contains tenofovir AF and emtricitabine, both of which are active against HBV) and can be used in renally impaired patients with creatinine clearance (CRCL) >/= 30 mL/min. Thus, although cost-effectiveness analyses would be beneficial, current data indicate that bictegravir/emtricitabine/tenofovir AF is a convenient initial and subsequent treatment option for adults with HIV-1 infection, including those co-infected with HBV, and provides the first non-pharmacologically boosted, INSTI-based, triple-combination STR suitable for patients with CRCL 30-50 mL/min.
DrugBank Data that Cites this Article
- Drugs
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Tenofovir alafenamide Liver carboxylesterase 1 Protein Humans NoSubstrateDetails Tenofovir alafenamide Lysosomal protective protein Protein NoSubstrateDetails - Drug Carriers
Drug Carrier Kind Organism Pharmacological Action Actions Tenofovir Serum albumin Protein Humans NoBinderDetails Tenofovir alafenamide Serum albumin Protein Humans NoBinderDetails - Drug Transporters
Drug Transporter Kind Organism Pharmacological Action Actions Tenofovir alafenamide ATP-binding cassette sub-family G member 2 Protein Humans NoSubstrateDetails