Comparative Pharmacology
Head-to-head clinical analysis: BICTEGRAVIR EMTRICITABINE AND TENOFOVIR ALAFENAMIDE versus EMTRICITABINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BICTEGRAVIR EMTRICITABINE AND TENOFOVIR ALAFENAMIDE versus EMTRICITABINE.
BICTEGRAVIR, EMTRICITABINE AND TENOFOVIR ALAFENAMIDE vs EMTRICITABINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Bictegravir is an HIV-1 integrase strand transfer inhibitor that blocks viral DNA integration into host genome. Emtricitabine is a nucleoside reverse transcriptase inhibitor that terminates viral DNA chain elongation. Tenofovir alafenamide is a nucleotide reverse transcriptase inhibitor that incorporates into viral DNA causing chain termination.
Nucleoside reverse transcriptase inhibitor; phosphorylated to emtricitabine triphosphate which competes with endogenous deoxycytidine triphosphate and incorporates into viral DNA causing chain termination.
One tablet (50 mg bictegravir, 200 mg emtricitabine, 25 mg tenofovir alafenamide) orally once daily.
200 mg orally once daily, typically in combination with other antiretroviral agents.
None Documented
None Documented
Bictegravir: 17.3 h (HIV-1 patients); Emtricitabine: 10 h (HIV-1 patients); Tenofovir alafenamide: 0.51 h (rapid conversion to tenofovir); Tenofovir (active metabolite): 32-37 h (cellular half-life in PBMCs).
Terminal elimination half-life is approximately 10 hours (range 8–12 hours) in adults with normal renal function; prolonged to >20 hours in severe renal impairment (CrCl <30 mL/min).
Bictegravir: 60% feces (as parent), 35% urine (as parent); Emtricitabine: 86% urine (70% unchanged, 14% metabolites), 14% feces; Tenofovir alafenamide: <1% urine (as parent), >80% feces (as tenofovir), renal elimination of tenofovir (through active tubular secretion) accounts for ~30-50% of a TAF dose.
Renal: approximately 86% of the dose is excreted unchanged in urine via glomerular filtration and active tubular secretion. Biliary/fecal: minimal (<14% as unchanged drug and metabolites in feces).
Category A/B
Category C
NRTI
Antiretroviral, NRTI