Comparative Pharmacology
Head-to-head clinical analysis: ATAZANAVIR SULFATE versus EVOTAZ.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ATAZANAVIR SULFATE versus EVOTAZ.
ATAZANAVIR SULFATE vs EVOTAZ
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Atazanavir is an azapeptide HIV-1 protease inhibitor. It selectively inhibits the virus-specific processing of viral Gag and Gag-Pol polyproteins in HIV-1 infected cells, preventing formation of mature virions.
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.
300 mg orally once daily with ritonavir 100 mg orally once daily, or 400 mg orally once daily without ritonavir (when used alone).
1 tablet (300 mg atazanavir and 150 mg cobicistat) orally once daily with food.
None Documented
None Documented
Terminal elimination half-life: ~6.5 to 7 hours; supports once-daily dosing.
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.
Biliary/fecal: ~79% as unchanged drug; renal: ~13% (including <1% unchanged).
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%.
Category C
Category C
Protease Inhibitor
Protease Inhibitor