Comparative Pharmacology
Head-to-head clinical analysis: APTIVUS versus TIVICAY PD.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APTIVUS versus TIVICAY PD.
APTIVUS vs TIVICAY PD
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.
Tivicay PD (dolutegravir) is an HIV-1 integrase strand transfer inhibitor (INSTI) that inhibits the catalytic activity of HIV-1 integrase, preventing the integration of viral DNA into host chromosomal DNA, which is essential for 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.
50 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 is approximately 12-15 hours in adults, supporting once-daily dosing.
Fecal (79.5% unchanged), renal (4.4% unchanged).
Primarily metabolized by UGT1A1 with minor CYP3A4; 53% of dose recovered in feces (30% as unchanged drug) and 31% in urine (18% as unchanged drug).
Category C
Category C
Antiretroviral
Antiretroviral, integrase inhibitor