Cabenuva Generic Name & Formulations
Cabotegravir ext-rel (200mg/mL), rilpivirine ext-rel (300mg/mL); 400mg/600mg, 600mg/900mg; per co-packaged kit; susp for IM inj.
HIV-1 integrase strand transfer inhibitor (INSTI) + non-nucleoside reverse transcriptase inhibitor.
Kit—1 (1 vial of cabotegravir + 1 vial of rilpivirine) w. supplies
Mechanism of Action
Cabotegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral deoxyribonucleic acid (DNA) integration which is essential for the HIV replication cycle. Rilpivirine inhibits HIV-1 replication by non-competitive inhibition of HIV-1 reverse transcriptase. It does not inhibit the human cellular DNA polymerases α, β and γ.
As a complete regimen for HIV-1 infection to replace the current antiretroviral regimen in patients who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine.
Cabenuva Dosage and Administration
Must be administered by a healthcare provider. Give each IM inj at separate gluteal inj sites (on opposite sides or 2cm apart) during same visit; preferably ventrogluteal site. Do not administer by any other route or anatomical site. ≥12yrs (≥35kg): Prior to initiation, may consider giving oral lead-in dosing (with Vocabria and Edurant) for approx. 1 month (≥28 days) to assess tolerability or may proceed directly to Cabenuva inj without use of an oral lead-in. Select appropriate inj dosing option. Monthly dosing: initiate single injections of 600mg/900mg (on the last day of current antiretroviral therapy or oral lead-in, if used), then continue single injections of 400mg/600mg once monthly onwards. Or, every 2-month dosing: initiate single injections of 600mg/900mg (on the last day of current antiretroviral therapy or oral lead-in, if used) consecutively 1 month apart for 2 months (Months 1 and 2), and then continue every 2 months onwards (starting at Month 4). Both regimens: may give injections up to 7 days before or after the scheduled date to receive monthly or every 2-month injections. Switching from monthly to every 2-month injections, every 2-month to monthly injections, missed injections: see full labeling.
<12yrs or <35kg: not established.
Concomitant carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifabutin, rifampin, rifapentine, systemic dexamethasone (more than 1 dose), St. John's wort.
Cabenuva Boxed Warnings
Discontinue immediately if hypersensitivity reactions develop. Monitor for post-inj reactions; treat appropriately if occur. Underlying liver disease or marked elevation in transaminases. Monitor liver function; discontinue if hepatotoxicity is suspected. Promptly evaluate if depressive symptoms occur. Long-acting properties: residual drug concentrations may remain ≥12months. Switch to an alternative regimen if virologic failure is suspected. Severe hepatic impairment. Severe renal impairment or ESRD: monitor. Elderly. Pregnancy: monitor. Nursing mothers: not recommended.
Time to maximum plasma concentration (median): 7 days (cabotegravir); 3–4 days (rilpivirine).
Plasma protein bound: >99.8% (cabotegravir); 99.7% (rilpivirine). Blood-to-plasma ratio: 0.52 (cabotegravir); 0.7 (rilpivirine). CSF-to-plasma concentration ratio (median): 0.003 (cabotegravir); 0.01 (rilpivirine).
Cabotegravir: UGT1A1, UGT1A9 (minor); rilpivirine: CYP3A.
Cabotegravir: fecal (59%), renal (27%); rilpivirine: fecal (85%), renal (6%). Half-life: 5.6–11.5 weeks (cabotegravir); 13–28 weeks (rilpivirine).
See Contraindications. Concomitant other antiretroviral drugs: not recommended. Cabotegravir: antagonized by strong UGT1A1 or 1A9 inducers. Rilpivirine: antagonized by CYP3A inducers or may be potentiated by CYP3A inhibitors. Concomitant drugs with a known risk for torsade de pointes (eg, azithromycin, clarithromycin, erythromycin); caution; consider alternatives. Concomitant methadone; monitor; may need dose adjustment.
Cabenuva Adverse Reactions
Inj site reactions, pyrexia, fatigue, headache, musculoskeletal pain, nausea, sleep disorders, dizziness, rash; hepatotoxicity, depressive disorders.
Cabenuva Clinical Trials
Cabenuva Patient Counseling