Comparative Pharmacology
Head-to-head clinical analysis: LEXIVA versus LOPINAVIR RITONAVIR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LEXIVA versus LOPINAVIR RITONAVIR.
LEXIVA vs LOPINAVIR; 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 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.
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 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
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: 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.
Renal (approximately 82% in urine, with 14% as parent drug and 68% as metabolites); fecal (approximately 16%, with 7% as parent drug).
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