Comparative Pharmacology
Head-to-head clinical analysis: APTIVUS versus FORTOVASE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APTIVUS versus FORTOVASE.
APTIVUS vs FORTOVASE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Tipranavir is a nonpeptidic HIV-1 protease inhibitor that binds to the active site of HIV-1 protease, thereby preventing the cleavage of viral polyprotein precursors into functional proteins, resulting in the production of immature, noninfectious viral particles.
Saquinavir is a protease inhibitor that binds to the active site of HIV-1 protease, blocking the cleavage of viral polyprotein precursors into functional proteins, resulting in the production of immature, non-infectious viral particles.
Oral: 500 mg twice daily with ritonavir 200 mg twice daily. Oral solution: 500 mg (1.25 mL) twice daily with ritonavir 200 mg twice daily. Must be taken with food.
1200 mg orally three times daily with food.
None Documented
None Documented
Terminal elimination half-life is 2.1 hours during multiple dosing with ritonavir (due to CYP3A inhibition), 5.5 hours when given alone.
Terminal elimination half-life is 1-2 hours in healthy subjects; prolonged to 2-5 hours in patients with hepatic impairment or when coadministered with ritonavir.
Fecal (79.5% unchanged), renal (4.4% unchanged).
Primarily hepatic metabolism via CYP3A4; 2% excreted unchanged in urine, 15% unchanged in feces; extensive biliary excretion of metabolites.
Category C
Category C
Antiretroviral
Antiretroviral