Comparative Pharmacology
Head-to-head clinical analysis: LEXIVA versus LOPINAVIR AND RITONAVIR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LEXIVA versus LOPINAVIR AND RITONAVIR.
LEXIVA vs LOPINAVIR AND RITONAVIR
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Fosamprenavir is a prodrug of amprenavir, a protease inhibitor (PI) that competitively inhibits HIV-1 protease, preventing cleavage of viral Gag-Pol polyprotein, resulting in immature, non-infectious viral particles.
Lopinavir is a HIV-1 protease inhibitor that prevents cleavage of viral Gag-Pol polyproteins, resulting in immature, non-infectious viral particles. Ritonavir is a potent CYP3A4 inhibitor that increases lopinavir plasma concentrations; at subtherapeutic doses, it also inhibits HIV-1 protease.
1400 mg orally twice daily (with ritonavir 100 mg) or 1400 mg orally once daily (with ritonavir 100 mg and cobicistat 150 mg). For treatment-naïve patients, 1400 mg orally once daily with ritonavir 100 mg or cobicistat 150 mg.
Lopinavir/ritonavir 400/100 mg (two tablets of 200/50 mg or 5 mL oral solution 80/20 mg per mL) orally twice daily with food.
None Documented
None Documented
Terminal elimination half-life is 2.8 to 5.7 hours; with ritonavir boosting, half-life increases to 7-10 hours, allowing once-daily dosing.
Lopinavir terminal elimination half-life is approximately 5–6 hours (range 4–8 h) when co-administered with ritonavir. Ritonavir half-life is about 3–5 hours. The prolonged half-life of lopinavir in the presence of ritonavir supports twice-daily dosing; steady state is reached within 2–3 days.
Renal (approximately 82% in urine, with 14% as parent drug and 68% as metabolites); fecal (approximately 16%, with 7% as parent drug).
Lopinavir is primarily eliminated via hepatic metabolism (CYP3A4), with <3% excreted unchanged in urine and ~20% excreted unchanged in feces. Ritonavir is also predominantly hepatically metabolized, with <3.5% excreted unchanged in urine and ~86% eliminated in feces (mostly as metabolites).
Category C
Category A/B
Protease Inhibitor
Protease Inhibitor