Overview
11 DESCRIPTION CABENUVA contains cabotegravir extended-release injectable suspension, an HIV INSTI, co-packaged with rilpivirine extended-release injectable suspension, an HIV NNRTI. Cabotegravir The chemical name for cabotegravir is ( 3S,11aR )-N-[(2,4-difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action CABENUVA contains 2 long-acting HIV-1 antiretroviral drugs, cabotegravir and rilpivirine [see Microbiology ( 12.4 )] . 12.2 Pharmacodynamics Cardiac Electrophysiology At a dose of cabotegravir 150 mg orally every 12 hours (10 times the recommended total daily oral lead-in dosage of CABENUVA), the QT interval is not prolonged to any clinically relevant extent. Administration of 3 doses of cabotegravir 150 mg orally every 12 hours resulted in a geometric mean C max approximately 2.8-, 5.4-, and 5.6-fold above the geometric mean steady-state C max associated with the recommended 30‑mg dose of oral cabotegravir, the recommended 400‑mg dose given monthly, and the recommended 600-mg dose given every 2 months of cabotegravir extended-release...
Indications
- 1 INDICATIONS AND USAGE CABENUVA is indicated as a complete regimen for the treatment of HIV-1 infection in adults and adolescents 12 years of age and older and weighing at least 35 kg to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA
Common Doses
- 600 mg
- 900 mg
- 400 mg
- 30 mg
Dosage
2 DOSAGE AND ADMINISTRATION • Refer to full prescribing information for detailed information on dosage and administration recommendations. ( 2 ) • Prior to initiating treatment with CABENUVA, oral lead-in dosing may be considered to assess the tolerability of cabotegravir and rilpivirine with the recommended dosage used for approximately 1 month. ( 2.3 ) • For gluteal intramuscular injection only. ( 2.4 , 2.5 , 2.9 ) • Recommended Monthly Dosing Schedule: Initiate injections of CABENUVA (600 mg of cabotegravir and 900 mg of rilpivirine) on the last day of current antiretroviral therapy or...
Contraindications
- 4 CONTRAINDICATIONS CABENUVA is contraindicated in patients: • with previous hypersensitivity reaction to cabotegravir or rilpivirine [see Warnings and Precautions ( 5.1 )] . • receiving the following coadministered drugs for which significant decreases in cabotegravir and/or rilpivirine plasma concentrations may occur due to uridine diphosphate glucuronosyltransferase (UGT)1A1 and/or cytochrome P450 (CYP)3A enzyme induction, which may result in loss of virologic response [see Drug Interactions ( 7 ), Clinical Pharmacology ( 12.
Side Effects
- 6 ADVERSE REACTIONS The following adverse reactions are described below and in other sections of the labeling: • Hypersensitivity reactions [see Warnings and Precautions ( 5.1 )] • Post-injection reactions [see Warnings and Precautions ( 5.2 )] • Hepatotoxicity [see Warnings and Precautions ( 5.3 )] • Depressive disorders [see Warnings and Precautions ( 5.4 )] The most common adverse reactions (Grades 1 to 4) observed in ≥2% of participants receiving CABENUVA were injection site reactions, pyrexia, fatigue, headache, musculoskeletal pain, nausea, sleep disorders, dizziness, and rash. ( 6.
Interactions
- 7 DRUG INTERACTIONS • Refer to the full prescribing information for important drug interactions with CABENUVA. ( 4 , 5.5 , 7 ) • Because CABENUVA is a complete regimen, coadministration with other antiretroviral medications for the treatment of HIV-1 infection is not recommended. ( 7.1 ) • Drugs that induce uridine diphosphate glucuronosyltransferase (UGT)1A1 or cytochrome P450 (CYP)3A4 may decrease the plasma concentrations of the components of CABENUVA. ( 4 , 7.3 , 7.4 ) • CABENUVA should be used with caution in combination with drugs with a known risk of Torsade de Pointes. ( 7.3 , 7.4 ) 7.