Comparative Pharmacology
Head-to-head clinical analysis: APTIVUS versus TIVICAY.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APTIVUS versus TIVICAY.
APTIVUS vs TIVICAY
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.
Dolutegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral DNA integration, which is essential for HIV 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.
50 mg orally once daily, or 50 mg twice daily when coadministered with potent UGT1A1 inducers (e.g., rifampin). For INSTI-naive patients: 50 mg once daily. For INSTI-experienced patients with suspected resistance: 50 mg twice daily.
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 approximately 14 hours (range 11-20 hours) in healthy subjects; supports once-daily dosing with a low pharmacokinetic boost.
Fecal (79.5% unchanged), renal (4.4% unchanged).
Primarily metabolized by UGT1A1 with minor CYP3A4 contribution; 53% of dose excreted in feces (31% as unchanged drug) and 33% in urine (1% unchanged).
Category C
Category C
Antiretroviral
Antiretroviral, integrase inhibitor