PURPOSE OF REVIEW Long-acting cabotegravir may provide a novel therapeutic option for both the treatment and prevention of HIV-1 infection that does not necessitate adherence to a daily regimen. The present review will highlight the unique formulation properties and pharmacologic attributes of long-acting cabotegravir nanosuspension. RECENT FINDINGS Cabotegravir is a potent integrase strand transfer inhibitor that has been formulated as an oral tablet for daily administration and as a long-acting injectable nanosuspension. Long-acting cabotegravir is readily absorbed following intramuscular and subcutaneous administration and has an elimination half-life of approximately 40 days, allowing for administration on a monthly or less frequent schedule. Repeat-dose pharmacokinetic studies and population pharmacokinetic modeling indicate monthly and bi-monthly dosing achieves clinically relevant plasma concentrations considered effective for HIV maintenance therapy and that quarterly injections are appropriate for investigation as preexposure prophylaxis. Cabotegravir is primarily metabolized by uridine diphosphate glucuronosyltransferase 1A1 and is unlikely to be impacted by the cytochrome P450 metabolic pathway. In vitro and in vivo data suggest cabotegravir has a low propensity to cause, or be subject to, significant drug interactions. SUMMARY The pharmacologic profile of long-acting cabotegravir supports its continued development for both treatment and prevention of HIV-1 infection.

中文翻译：

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长效cabotegravir的配方和药理作用。

审查的目的长效卡博可韦可能为治疗和预防HIV-1感染提供了一种新颖的治疗选择，不需要坚持每天的治疗方案。本文将重点介绍长效cabotegravir纳米混悬剂的独特制剂特性和药理特性。最新发现Cabotegravir是一种有效的整合酶链转移抑制剂，已被配制为每日给药的口服片剂和长效可注射的纳米混悬剂。长效cabotegravir在肌肉内和皮下给药后易于吸收，消除半衰期约为40天，可按月或更频繁地给药。重复剂量药代动力学研究和群体药代动力学模型表明，每月一次和每两月一次给药可达到被认为对HIV维持疗法有效的临床相关血浆浓度，并且每季度注射一次适合作为暴露前预防的研究对象。Cabotegravir主要由尿苷二磷酸葡萄糖醛酸糖基转移酶1A1代谢，不太可能受到细胞色素P450代谢途径的影响。体外和体内数据表明，cabotegravir引起或受到重大药物相互作用的可能性很低。概述长效卡博可韦的药理学特征支持其在治疗和预防HIV-1感染方面的持续发展。