Comparative Pharmacology
Head-to-head clinical analysis: APRETUDE versus APTIVUS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APRETUDE versus APTIVUS.
APRETUDE vs APTIVUS
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Apretude (cabotegravir) is an HIV-1 integrase strand transfer inhibitor (INSTI) that inhibits the integration of HIV-1 DNA into host genomic DNA, which is essential for viral replication. It binds to the active site of integrase and blocks the strand transfer step of retroviral DNA integration.
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.
600 mg IM every 2 months, initiated as two consecutive monthly loading doses of 600 mg each, for HIV-1 pre-exposure prophylaxis.
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.
None Documented
None Documented
Terminal elimination half-life is approximately 40 hours following subcutaneous injection, supporting monthly dosing.
Terminal elimination half-life is 2.1 hours during multiple dosing with ritonavir (due to CYP3A inhibition), 5.5 hours when given alone.
Renal (approximately 30% as unchanged drug) and fecal (approximately 50% as metabolites and unchanged drug) following oral administration.
Fecal (79.5% unchanged), renal (4.4% unchanged).
Category C
Category C
Antiretroviral
Antiretroviral