Comparative Pharmacology
Head-to-head clinical analysis: DARUNAVIR versus EVOTAZ.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DARUNAVIR versus EVOTAZ.
DARUNAVIR vs EVOTAZ
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Darunavir is an HIV-1 protease inhibitor that selectively inhibits the cleavage of HIV-1 encoded Gag-Pol polyproteins in virus-infected cells, thereby preventing formation of mature infectious 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.
600 mg orally twice daily with ritonavir 100 mg twice daily or 800 mg orally once daily with cobicistat 150 mg once daily, taken with food.
1 tablet (300 mg atazanavir and 150 mg cobicistat) orally once daily with food.
None Documented
None Documented
Clinical Note
moderateDarunavir + Tenofovir disoproxil
"The serum concentration of Tenofovir disoproxil can be increased when it is combined with Darunavir."
Clinical Note
moderateDarunavir + Sulfisoxazole
"The metabolism of Sulfisoxazole can be decreased when combined with Darunavir."
Clinical Note
moderateDarunavir + Fluconazole
"The metabolism of Fluconazole can be decreased when combined with Darunavir."
Clinical Note
moderateDarunavir + Clotrimazole
Terminal elimination half-life is approximately 15 hours when co-administered with low-dose ritonavir, supporting 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.
Primarily fecal (79.5% as unchanged drug or metabolites), with renal excretion accounting for approximately 13.9% (8.9% 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 A/B
Category C
Protease Inhibitor
Protease Inhibitor
"The metabolism of Clotrimazole can be decreased when combined with Darunavir."