Whitfield T, et al. – In this paper, evidence to date were summarized regarding the profile of cabotegravir and its potential in the treatment and prevention of HIV–1 infection. As per findings, cabotegravir appeared as a new member of the integrase strand transfer inhibitor class with potential for alternative mode of delivery. Researchers seemed to look for Phase III studies to define its efficacy and real–world experience to learn which patient groups stand to benefit most from the novel mode of delivery of treatment and preexposure prophylaxis (PrEP).

• Cabotegravir was identified as an integrase strand transfer inhibitor and an analog of dolutegravir.
• Unlike dolutegravir, cabotegravir seemed to have a long half–life and could be formulated into a long–acting nanosuspension for parenteral administration.
• As per initial pharmokinetic studies in humans, adequate drug levels were achieved with intramuscular (IM) administration at 4 weekly and 8 weekly intervals, with few interactions with commonly used concomitant medications.
• Preliminary animal PrEP studies suggested that IM cabotegravir has the potential to prevent simian/HIV acquisition from rectal, vaginal, and intravenous challenge.
• Two ongoing Phase II studies assessing cabotegravir as a PrEP agent in humans were identified: ÉCLAIR and HPTN077.
• Researchers studied cabotegravir in combination with rilpivirine as long–acting IM maintenance therapy.
• Results from the Long–Acting Antiretroviral Treatment Enabling study established that those switching to oral cabotegravir/rilpivirine once virologically suppressed were more likely to maintain suppression than those continuing standard efavirenz–based therapy (82% vs 71% at 24 weeks).
• Initial results of the Long–Acting Antiretroviral Treatment Enabling–2 study of parenteral regimens indicated that 12 weeks after randomization to parenteral or oral regimens, no difference was observed in proportions virologically suppressed on cabotegravir/rilpivirine daily orally vs IM every 4 weeks or 8 weeks (91% vs 94% vs 95%).
• Despite injection site pain in most recipients, the injections were well tolerated, most participants reported satisfaction with parenteral therapy.