Comparative Pharmacology
Head-to-head clinical analysis: ATAZANAVIR SULFATE versus DARUNAVIR AND RITONAVIR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ATAZANAVIR SULFATE versus DARUNAVIR AND RITONAVIR.
ATAZANAVIR SULFATE vs DARUNAVIR AND RITONAVIR
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 a protease inhibitor that binds to the HIV-1 protease active site, preventing cleavage of viral polyproteins into functional proteins, leading to immature, non-infectious virions. Ritonavir is a potent CYP3A4 inhibitor that increases darunavir plasma concentrations by inhibiting its metabolism.
300 mg orally once daily with ritonavir 100 mg orally once daily, or 400 mg orally once daily without ritonavir (when used alone).
Darunavir 800 mg orally once daily plus ritonavir 100 mg orally once daily in treatment-naïve patients. In treatment-experienced patients with at least one darunavir resistance-associated mutation, darunavir 600 mg plus ritonavir 100 mg orally twice daily.
None Documented
None Documented
Terminal elimination half-life: ~6.5 to 7 hours; supports once-daily dosing.
Darunavir: ~15 hours (range 10-31 h) when boosted with ritonavir; allows once-daily dosing. Ritonavir: ~3-5 hours (administered as booster).
Biliary/fecal: ~79% as unchanged drug; renal: ~13% (including <1% unchanged).
Darunavir: 79.5% fecal (primarily as unchanged drug), 13.9% renal (mostly metabolites). Ritonavir: 86.4% fecal, 11.3% renal.
Category C
Category A/B
Protease Inhibitor
Protease Inhibitor