Comparative Pharmacology
Head-to-head clinical analysis: ELVITEGRAVIR COBICISTAT EMTRICITABINE AND TENOFOVIR ALAFENAMIDE versus EMTRICITABINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ELVITEGRAVIR COBICISTAT EMTRICITABINE AND TENOFOVIR ALAFENAMIDE versus EMTRICITABINE.
ELVITEGRAVIR, COBICISTAT, EMTRICITABINE AND TENOFOVIR ALAFENAMIDE vs EMTRICITABINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Elvitegravir is an HIV-1 integrase strand transfer inhibitor, blocking viral DNA integration. Cobicistat is a CYP3A inhibitor boosting elvitegravir exposure. Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI). Tenofovir alafenamide is a nucleotide reverse transcriptase inhibitor (NtRTI) that, after conversion to tenofovir, inhibits HIV reverse transcriptase.
Nucleoside reverse transcriptase inhibitor; phosphorylated to emtricitabine triphosphate which competes with endogenous deoxycytidine triphosphate and incorporates into viral DNA causing chain termination.
One tablet (150 mg elvitegravir, 150 mg cobicistat, 200 mg emtricitabine, 10 mg tenofovir alafenamide) orally once daily with food.
200 mg orally once daily, typically in combination with other antiretroviral agents.
None Documented
None Documented
Elvitegravir: 12.9 h; Cobicistat: 3.5 h; Emtricitabine: 10 h; Tenofovir alafenamide: 0.51 h (active metabolite tenofovir has half-life of 12-18 h). All half-lives are terminal elimination half-lives; once-daily dosing is supported by boosted pharmacokinetics.
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).
Elvitegravir: 94% fecal, 6.7% renal; Cobicistat: 86% fecal, 8% renal; Emtricitabine: 86% renal (unchanged); Tenofovir alafenamide: 31% renal (as tenofovir), 46% fecal (as tenofovir alafenamide).
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