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Cabotegravir/Rilpivirine

    Brands

    DEA Class; Rx

    Common Brand Names; Cabenuva

    • HIV, Integrase Inhibitors; 
    • HIV, NNRTIs

    Cabotegravir: HIV-1 integrase strand transfer inhibitor (INSTI); cabotegravir, an analog of dolutegravir, prevents viral DNA integration into the host genome and inhibits HIV replication

    Rilpivirine: Non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1; inhibits HIV-1 replication by noncompetitive inhibition of HIV-1 reverse transcriptase

    Cabotegravir and rilpivirine are copackaged as 2 separate IM injections

    Indicated as a complete regimen for treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults and adolescents to replace a current stable antiretroviral therapy (ART) regimen in those who are virologically suppressed (HIV-1 RNA <50 copies/mL) with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine

    Documented hypersensitivity

    Injection site reactions, all grades (83%)

    Injection site reactions, ≥Grade 2 (37%)

    • Pyrexia (8%)
    • Fatigue (5%)
    • Headache (4%)
    • Musculoskeletal pain (3%)
    • Nausea (3%)
    • Sleep disorders (2%)
    • Dizziness (2%)
    • Rash (2%)
    • Pyrexia (2%)
    • Fatigue (1%)
    • Musculoskeletal pain (1%)
    • Creatine phosphokinase ≥10 x ULN (8%)
    • Lipase ≥3 x ULN (5%)
    • ALT/AST ≥5 x ULN (2%)

    Serious postinjection reactions were reported within minutes after injection of rilpivirine, including dyspnea, agitation, abdominal cramping, flushing, sweating, oral numbness, and changes in blood pressure; symptoms began to resolve within a few minutes after injection; these events may have been associated with inadvertent (partial) IV administration; observe patient for 10 minutes after injection

    Hepatotoxicity reported in patients with or without known preexisting hepatic disease or known risk factors; monitoring of liver chemistries recommended; discontinue treatment if hepatotoxicity suspected

    Depressive disorders (including depressed mood, depression, mood altered, mood swings) reported; promptly evaluate if symptoms emerge; determine whether risks of continued therapy outweigh benefits

    To minimize the potential risk of developing viral resistance, it is essential to initiate an alternative, fully suppressive antiretroviral regimen ≤1 month after final injections when dosed monthly and ≤2 months after final injections when dosed every 2 months; if virologic failure is suspected, switch to an alternative regimen as soon as possible

    Data are insufficient regarding use during pregnancy to adequately assess drug-associated risk of birth defects and miscarriage

    While there are insufficient human data to assess the risk of neural tube defects (NTDs) with exposure to cabotegravir during pregnancy, NTDs were associated with dolutegravir, another integrase inhibitor

    Unknown if present in human breast milk, affects human milk production, or effects on breastfed infants

    CDC recommends that women in the United States should not breastfeed their infants because of risk of the following H4

    Adults

    Optional oral lead-in dosing

    • May use oral lead-in for ~1 month (at least 28 days) before initiating to assess tolerability of cabotegravir and rilpivirine for monthly- or every-2-month dosage regimens
    • Cabotegravir (Vocabria) 30 mg plus rilpivirine (Edurant) 25 mg qDay for ~1 month (at least 28 days) to ensure medications are well tolerated

    Once-monthly regimen

    • Administer each drug as 2 separate IM injections
    • One-time initiating injection
      • Initiate on last day of current ART therapy or oral lead-in (if used)
      • Cabotegravir 600 mg (3 mL) IM PLUS
      • Rilpivirine 900 mg (3 mL) IM
    • Continuation injections every month
      • Administer once monthly after initial injections
      • Cabotegravir 400 mg (2 mL) IM qMonth PLUS
      • Rilpivirine 600 mg (2 mL) IM qMonth
      • Give up to 7 days before or after scheduled monthly injections

    Every 2-month regimen

    • Administer each drug as 2 separate IM injections
    • Initiating injections
      • Initiate on last day of current ART therapy or oral lead-in (if used)
      • Cabotegravir 600 mg (3 mL) IM qMonth x 2 PLUS
      • Rilpivirine 900 mg (3 mL) IM qMonth x 2
      • Give up to 7 days before or after scheduled second initiation injections
    • Continuation injections every 2 months
      • Initiate at Month 3, and then every 2 months thereafter
      • Cabotegravir 600 mg (3 mL) IM every 2 months PLUS
      • Rilpivirine 900 mg (3 mL) IM every 2 months
      • Give up to 7 days before or after scheduled injections

    Cabotegravir and rilpivirine are copackaged as 2 separate IM injections

    Each dosing kit also contains 2 syringes, 2 syringe labels, 2 vial adapters, and 2 needles for IM injection (23-gauge, 1.5-inch)

    Vial stoppers are not made with natural rubber latex

    injection, IM suspension 400mg/600mg kit

    • Cabotegravir: 400mg/2mL
    • Rilpivirine: 600mg/2mL

    injection, IM suspension 600mg/900mg kit

    • Cabotegravir: 600mg/3mL
    • Rilpivirine: 900mg/3mL