Apretude Generic Name & Formulations
Cabotegravir ext-rel 600mg/3mL (200mg/mL); per vial; susp for IM inj.
HIV-1 integrase strand transfer inhibitor (INSTI).
Kit—1 (vial 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.
For pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection in at-risk adults and adolescents.
Apretude Dosage and Administration
Prior to initiation (with or without an oral cabotegravir lead-in) and each subsequent inj, must have a negative HIV-1 test. Must be administered by a healthcare provider. Give each IM inj at gluteal inj sites. Do not administer by any other route or anatomical site. ≥12yrs (≥35kg): Initiate injections at 600mg once on Months 1 and 2; continue at 600mg every 2 months starting on Month 4 onwards (may be given up to 7 days before or after the scheduled date to receive injections). With oral lead-in (cabotegravir for at least 28 days): initiate injections (on the last day of oral lead-in or within 3 days thereafter) at 600mg once on Months 2 and 3; continue at 600mg every 2 months starting on Month 5 onwards (may be given up to 7 days before or after the scheduled date to receive injections). Concomitant rifabutin (started before or with the 1st inj): initiate injections at 600mg once, repeat dose 2 weeks later, and then monthly thereafter while on rifabutin; (started with 2nd inj or later): 600mg monthly while on rifabutin. Missed injections: see full labeling.
<12yrs or <35kg: not established.
Unknown or positive HIV-1 status. Concomitant carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, rifapentine.
Apretude Boxed Warnings
Risk of drug resistance with use of Apretude for HIV-1 pre-exposure prophylaxis (PrEP) in undiagnosed HIV-1 infection.
Provide comprehensive management to reduce the risk of HIV-1 acquisition. Counsel individuals on the use of other prevention measures (eg, condom use, knowledge of partner(s)’ HIV-1 status, regular testing for STIs). Potential risk of resistance: reassess for HIV-1 acquisition risk; test before each inj to confirm HIV-1 negative status. Discontinue immediately if hypersensitivity reactions occur. Monitor liver function; discontinue if hepatotoxicity is suspected. Promptly evaluate if depressive symptoms occur. Long-acting properties: residual drug concentrations may remain ≥12months. Severe hepatic impairment. Severe renal impairment or ESRD: monitor. Elderly. Pregnancy. Nursing mothers: assess benefit/risk to infant.
Median time to reach maximum concentration: 7 days.
Plasma protein bound: >99.8%. Blood-to-plasma ratio: 0.52. CSF-to-plasma concentration ratio (median [range]): 0.003 (0.002 to 0.004).
UGT1A1, UGT1A9 (minor).
Fecal (59%), renal (27%). Half-life: 5.6–11.5 weeks.
See Contraindications. Antagonized by strong UGT1A1 or 1A9 inducers. Antagonized by rifabutin (see Adult dose).
Apretude Adverse Reactions
Inj site reactions, diarrhea, headache, pyrexia, fatigue, sleep disorders, nausea, dizziness, flatulence, abdominal pain, vomiting, myalgia, rash, decreased appetite, somnolence, back pain, upper respiratory tract infection; hepatotoxicity, depressive disorders.
Apretude Clinical Trials
Apretude Patient Counseling