Comparative Pharmacology
Head-to-head clinical analysis: ATAZANAVIR SULFATE versus DARUNAVIR ETHANOLATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ATAZANAVIR SULFATE versus DARUNAVIR ETHANOLATE.
ATAZANAVIR SULFATE vs DARUNAVIR ETHANOLATE
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.
Darunavir is an HIV-1 protease inhibitor that selectively inhibits the cleavage of HIV-encoded Gag-Pol polyproteins in infected cells, thereby preventing the formation of mature infectious virus particles.
300 mg orally once daily with ritonavir 100 mg orally once daily, or 400 mg orally once daily without ritonavir (when used alone).
600 mg orally twice daily with ritonavir 100 mg twice daily, or 800 mg orally once daily with ritonavir 100 mg once daily and with food.
None Documented
None Documented
Terminal elimination half-life: ~6.5 to 7 hours; supports once-daily dosing.
Terminal elimination half-life is approximately 15 hours when coadministered with ritonavir (100 mg), and about 5-6 hours without booster. Clinical context: allows once-daily or twice-daily dosing with boosting.
Biliary/fecal: ~79% as unchanged drug; renal: ~13% (including <1% unchanged).
Primarily hepatic metabolism via CYP3A4, followed by biliary excretion of metabolites; renal excretion of unchanged drug is minimal (<10%). In feces, approximately 79% of dose is recovered as metabolites; in urine, <10% as unchanged drug.
Category C
Category A/B
Protease Inhibitor
Protease Inhibitor