Comparative Pharmacology
Head-to-head clinical analysis: ELVITEGRAVIR COBICISTAT EMTRICITABINE AND TENOFOVIR ALAFENAMIDE versus EMTRIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ELVITEGRAVIR COBICISTAT EMTRICITABINE AND TENOFOVIR ALAFENAMIDE versus EMTRIVA.
ELVITEGRAVIR, COBICISTAT, EMTRICITABINE AND TENOFOVIR ALAFENAMIDE vs EMTRIVA
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; emtricitabine is phosphorylated to emtricitabine 5'-triphosphate which competes with deoxycytidine 5'-triphosphate for incorporation into viral DNA, resulting in chain termination.
One tablet (150 mg elvitegravir, 150 mg cobicistat, 200 mg emtricitabine, 10 mg tenofovir alafenamide) orally once daily with food.
Emtricitabine 200 mg orally once daily.
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 ~10 hours (mean 10 h, range 7-14 h) in adults; prolonged in renal impairment (up to 90 h in severe impairment)
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 excretion of unchanged drug (~86%) by glomerular filtration and active tubular secretion; fecal excretion (<1%)
Category A/B
Category C
NRTI
Antiretroviral, NRTI