Apretude (cabotegravir) long-acting injection is now available for HIV PrEP

ViiV Healthcare is introducing Apretude (cabotegravir 30 mg tablets and cabotegravir 600 mg/3mL extended-release injectable suspension), the first injectable for HIV prevention in Canada. It is indicated for at-risk adults and adolescents (age ≥ 12 years and weighing ≥ 35 kg) for pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection.1Cabotegravir inhibits HIV integrase. This leads to blockage of the strand transfer step of retroviral deoxyribonucleic acid (DNA) integration, which is essential for the HIV replication cycle.1 Following a dose of the long-acting injection, the time to maximum concentration is seven days. The terminal elimination half-life is 5.6–11.5 weeks. Following discontinuation, the drug is detectable in the plasma for up to a year or longer.1Cabotegravir injection may be initiated with or without a cabotegravir oral lead-in. The oral lead-in is used to assess tolerability to cabotegravir before starting cabotegravir extended-release injections. The tablets may also be used if a dose of injection is missed or delayed, until the patient is able to receive injections again.1 When an oral lead-in is used, dosing consists of three phases: Oral lead-in with cabotegravir tablets—30 mg once daily for approximately one month (at least 28 days)Initiation of cabotegravir injection on the last day of oral lead-in (or within 3 days thereafter). A single 3 mL (600 mg) intramuscular (gluteal) injection is given, followed by a second 3 mL (600 mg) intramuscular injection one month later (up to 7 days before or after the scheduled dose)Continuation of cabotegravir injections (3 mL [600 mg] every 2 months), administered up to seven days before or after the scheduled injection visit.1 When starting with Apretude injection directly (i.e., without an oral lead-in), the first and second injections (600 mg/3 mL) are given one month apart, the third injection two months after the second dose, and subsequent injections every two months thereafter. No dosage adjustment is required in individuals with mild to severe renal impairment, or mild or moderate hepatic impairment. 1Apretude tablets may be administered with or without food. For the injection, the vial must be shaken vigorously before drawing the suspension into the syringe. The injection should be administered as soon as possible after the syringe is prepared, but may remain in the syringe for up to two hours at room temperature.1 Administer the injection by intramuscular (gluteal) injection.1 A ventrogluteal site is recommended, but dorsogluteal injection (upper outer quadrant) is acceptable, if preferred by the healthcare professional. Consider the body mass index (BMI) of the individual to ensure that the needle length is sufficient to reach the gluteus muscle. Longer needles (not included in the dosing kit) may be required for individuals with higher BMI (> 30 kg/m2) to ensure that the injection is administered intramuscularly (not subcutaneously).2 Injection site reactions, including pain, tenderness, nodules, induration and swelling, are the most common adverse effects of cabotegravir injections. Headache, diarrhea and pyrexia may also occur with the tablets or injections.1 Cases of hepatotoxicity, presenting as serum transaminase elevations, have occurred in individuals with or without pre-existing hepatic disease or other identifiable risk factors. Depressive disorders have been reported and hypersensitivity reactions are possible.1 There is a risk of drug resistance with cabotegravir use in undiagnosed HIV-1 infection; individuals must be tested for HIV-1 infection before starting therapy and with each subsequent injection. Patients should be counselled to strictly adhere to the recommended dosing schedule, to reduce the risk of HIV-1 acquisition and the potential development of resistance.1 Regarding drug interactions, cabotegravir is contraindicated with anticonvulsants (carbamazepine, oxcarbazepine, phenobarbital, phenytoin), rifampin and rifapentine; these agents may significantly reduce cabotegravir concentrations. Administer antacids at least two hours before or four hours after taking cabotegravir tablets, as antacids may also reduce cabotegravir concentrations. Consult the product monograph for management of interactions with rifabutin.1Apretude film-coated tablets are supplied quantities of 30, in bottles with child-resistant closures. Apretude injection is supplied as a kit containing one 600 mg/3 mL single-dose vial of cabotegravir extended release injectable suspension. The kit also contains one syringe, one syringe adaptor and one needle for intramuscular injection (23-gauge, 1.5-inch).1Apretude (cabotegravir tablets and cabotegravir extended-release injectable suspension) is the first long-acting injectable for HIV prevention in Canada.3 Cabotegravir is also available in Canada as Vocabria (cabotegravir tablet), an oral lead-in to Cabenuva (cabotegravir ER injectable suspension and rilpivirine ER suspension). Vocabria/Cabenuva is indicated as a complete regimen for the treatment of HIV-1 infection; it is not indicated for HIV prevention.4 References1. ViiV Healthcare ULC. Apretude (cabotegravir tablets and cabotegravir extended-release injectable suspension) product monograph. Montreal, QC; May 10, 2024. (accessed July 23, 2024).2. ViiV Healthcare. Apretude (cabotegravir extended-release injectable suspension). Full prescribing information (US). Durham, NC; December 2023. (accessed July 23, 2024).3. CATIE. Health Canada approves Apretude, the first long-acting injectable for HIV prevention. May 15, 2024. (accessed July 23, 2024).4. ViiV Healthcare ULC. Vocabria (cabotegravir tablets) and Cabenuva (cabotegravir extended-release injectable suspension and rilpivirine extended-release injectable suspension) product monograph. Montreal, QC; November 22, 2023. (accessed July 23, 2024).

Apretude (cabotegravir) long-acting injection is now available for HIV PrEP

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