General Information

Apretude (cabotegravir) is an HIV-1 integrase strand transfer inhibitor (INSTI).

Apretude is specifically indicated in at-risk adults and adolescents weighing at least 35 kg for pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection. Individuals must have a negative HIV-1 test prior to initiating APRETUDE (with or without an oral lead-in with oral cabotegravir) for HIV-1 PrEP.

Apretude is supplied as an injectable suspension for intramuscular use. Apretude contains cabotegravir extended-release injectable suspension in a single-dose vial. Apretude must be administered by a healthcare provider by gluteal intramuscular injection. Apretude may be initiated with oral cabotegravir prior to the intramuscular injections or the patient may proceed directly to injection of Apretude without an oral lead-in.

Apretude can be given as few as six times per year and is initiated with a single 600 mg (3-ml) injection given one month apart for two consecutive months. After the second initiation injection, the recommended continuation injection dose is a single 600 mg (3-ml) injection given every two months.

Side Effects

Adverse effects associated with the use of Apretude may include, but are not limited to, the following:

injection 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

Clinical Trial Results

FDA approval was based on the results from two, international phase IIb/III multicenter, randomized, double-blind, active controlled trials, HPTN 083 and HPTN 084 which evaluated the safety and efficacy of cabotegravir long-acting for PrEP in HIV-negative men who have sex with men, transgender women, and cisgender women, who were at increased risk of sexually acquiring HIV. In these trials, which included more than 7,700 participants across 13 countries combined, the blinded, randomized portions of both trials were stopped early by an independent Data Safety Monitoring Board after cabotegravir long-acting for PrEP was shown to be superior to daily oral emtricitabine/tenofovir disoproxil fumarate (TDF/FTC) tablets in preventing the acquisition of HIV in study participants. Clinical trial participants who received cabotegravir long-acting for PrEP experienced a 70% lower incidence of HIV compared to FTC/TDF tablets in HPTN 083 and a 90% lower incidence of HIV compared to FTC/TDF tablets in HPTN 084.