Comparative Pharmacology
Head-to-head clinical analysis: EVOTAZ versus LOPINAVIR RITONAVIR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EVOTAZ versus LOPINAVIR RITONAVIR.
EVOTAZ vs LOPINAVIR; RITONAVIR
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.
Lopinavir is an HIV-1 protease inhibitor that prevents cleavage of viral Gag-Pol polyprotein precursors, resulting in immature, non-infectious viral particles. Ritonavir is a potent CYP3A4 inhibitor used at low doses to boost lopinavir plasma levels.
1 tablet (300 mg atazanavir and 150 mg cobicistat) orally once daily with food.
Lopinavir 400 mg / Ritonavir 100 mg (two tablets or 5 mL oral solution) orally twice daily with food. Alternatively, once-daily dosing (800/200 mg) may be used in treatment-naïve patients with <3 lopinavir resistance mutations.
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.
Lopinavir: 5-6 hours; Ritonavir: 3-5 hours. When coadministered, ritonavir inhibits lopinavir metabolism, resulting in a prolonged lopinavir half-life (~5-6 hours) allowing twice-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%.
Primarily hepatic metabolism via CYP3A4; fecal excretion of metabolites (approximately 82-90%); renal excretion of unchanged drug is negligible (<3%).
Category C
Category A/B
Protease Inhibitor
Protease Inhibitor