Comparative Pharmacology
Head-to-head clinical analysis: APTIVUS versus VIRAC REX.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APTIVUS versus VIRAC REX.
APTIVUS vs VIRAC REX
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.
VirAcRex is a direct-acting antiviral that inhibits the viral RNA-dependent RNA polymerase (NS5B) by acting as a chain terminator, thereby blocking viral replication.
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.
300 mg orally once daily with or without 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: 2.5-3.5 hours; clinical context: requires thrice-daily dosing to maintain therapeutic levels.
Fecal (79.5% unchanged), renal (4.4% unchanged).
Renal: 30-40% unchanged; biliary/fecal: 50-60% as metabolites; <10% in feces as parent drug.
Category C
Category C
Antiretroviral
Antiretroviral