Comparative Pharmacology
Head-to-head clinical analysis: EVOTAZ versus LEXIVA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EVOTAZ versus LEXIVA.
EVOTAZ vs LEXIVA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
EVOTAZ is a fixed-dose combination of atazanavir, an HIV-1 protease inhibitor, and cobicistat, a CYP3A inhibitor. Atazanavir inhibits HIV-1 protease, preventing cleavage of viral polyproteins and resulting in immature, non-infectious virions. Cobicistat increases systemic exposure of atazanavir by inhibiting CYP3A-mediated metabolism.
Fosamprenavir is a prodrug of amprenavir, a protease inhibitor (PI) that competitively inhibits HIV-1 protease, preventing cleavage of viral Gag-Pol polyprotein, resulting in immature, non-infectious viral particles.
1 tablet (300 mg atazanavir and 150 mg cobicistat) orally once daily with food.
1400 mg orally twice daily (with ritonavir 100 mg) or 1400 mg orally once daily (with ritonavir 100 mg and cobicistat 150 mg). For treatment-naïve patients, 1400 mg orally once daily with ritonavir 100 mg or cobicistat 150 mg.
None Documented
None Documented
Cobicistat: terminal half-life approximately 3–4 hours; atazanavir: terminal half-life approximately 7 hours (range 5–12 hours) at steady state when boosted with cobicistat. The short half-life of cobicistat necessitates once-daily dosing with atazanavir to maintain therapeutic concentrations.
Terminal elimination half-life is 2.8 to 5.7 hours; with ritonavir boosting, half-life increases to 7-10 hours, allowing once-daily dosing.
Cobicistat: primarily hepatic metabolism (CYP3A4) and biliary/fecal excretion; <7% excreted unchanged renally. Atazanavir: primarily biliary/fecal excretion as unchanged drug and metabolites (79–88%); renal excretion accounts for <7%.
Renal (approximately 82% in urine, with 14% as parent drug and 68% as metabolites); fecal (approximately 16%, with 7% as parent drug).
Category C
Category C
Protease Inhibitor
Protease Inhibitor