Comparative Pharmacology
Head-to-head clinical analysis: BICTEGRAVIR EMTRICITABINE AND TENOFOVIR ALAFENAMIDE versus EMTRIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BICTEGRAVIR EMTRICITABINE AND TENOFOVIR ALAFENAMIDE versus EMTRIVA.
BICTEGRAVIR, EMTRICITABINE AND TENOFOVIR ALAFENAMIDE vs EMTRIVA
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; emtricitabine is phosphorylated to emtricitabine 5'-triphosphate which competes with deoxycytidine 5'-triphosphate for incorporation into viral DNA, resulting in chain termination.
One tablet (50 mg bictegravir, 200 mg emtricitabine, 25 mg tenofovir alafenamide) orally once daily.
Emtricitabine 200 mg orally once daily.
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 ~10 hours (mean 10 h, range 7-14 h) in adults; prolonged in renal impairment (up to 90 h in severe impairment)
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 excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Category A/B
Category C
NRTI
Antiretroviral, NRTI