Bictegravir, cabotegravir, dolutegravir, elvitegravir, and raltegravir are members of the latest class of antiretrovirals available to treat human immunodeficiency virus (HIV) infection, the integrase strand transfer inhibitors. Integrase strand transfer inhibitors are potent inhibitors of the HIV integrase enzyme with IC_90/95 values in the low nanogram per milliliter range and they retain antiviral activity against strains of HIV with acquired resistance to other classes of antiretrovirals. Each of the integrase strand transfer inhibitors have unique pharmacokinetic/pharmacodynamic properties, influencing their role in clinical use in specific subsets of patients. Cabotegravir, approved for use in Canada but not yet by the US Food and Drug Administration, is formulated in both oral and intramuscular formulations; the latter of which has shown efficacy as a long-acting extended-release formulation. Cabotegravir, raltegravir, and dolutegravir have minimal drug–drug interaction profiles, as their metabolism has minimal cytochrome P450 involvement. Conversely, elvitegravir metabolism occurs primarily via cytochrome P450 3A4 and requires pharmacokinetic boosting to achieve systemic exposures amenable to once-daily dosing. Bictegravir metabolism has similar contributions from both cytochrome P450 3A4 and uridine 5ʹ-diphospho-glucuronosyltransferase 1A1. Bictegravir, dolutegravir, and raltegravir are recommended components of initial regimens for most people with HIV in the US adult and adolescent HIV treatment guidelines. This review summarizes and compares the pharmacokinetics and pharmacodynamics of the integrase strand transfer inhibitor agents, and describes specific pharmacokinetic considerations for persons with hepatic impairment, renal dysfunction, pregnancy, and co-infections.

Bictegravir、cabotegravir、dolutegravir、elvitegravir 和 raltegravir 是可用于治疗人类免疫缺陷病毒 (HIV) 感染的最新一类抗逆转录病毒药物，即整合酶链转移抑制剂。整合酶链转移抑制剂是 HIV 整合酶的有效抑制剂，IC 为_90/95值在低纳克/毫升范围内，并且它们保留了对 HIV 毒株的抗病毒活性，这些毒株对其他类别的抗逆转录病毒药物具有获得性耐药性。每种整合酶链转移抑制剂都具有独特的药代动力学/药效学特性，影响了它们在特定患者亚群的临床应用中的作用。Cabotegravir 已获准在加拿大使用，但尚未获得美国食品和药物管理局的批准，可制成口服和肌肉注射制剂；后者已显示出作为长效缓释制剂的功效。Cabotegravir、raltegravir 和 dolutegravir 具有最小的药物相互作用特征，因为它们的代谢对细胞色素 P450 的参与最小。反过来，elvitegravir 代谢主要通过细胞色素 P450 3A4 发生，需要加强药代动力学以实现适合每日一次给药的全身暴露。Bictegravir 代谢对细胞色素 P450 3A4 和尿苷 5ʹ-二磷酸-葡萄糖醛酸基转移酶 1A1 的作用相似。在美国成人和青少年 HIV 治疗指南中，Bictegravir、dolutegravir 和 raltegravir 是大多数 HIV 感染者初始治疗方案的推荐成分。本综述总结并比较了整合酶链转移抑制剂药物的药代动力学和药效学，并描述了肝功能损害、肾功能不全、妊娠和合并感染患者的具体药代动力学注意事项。Bictegravir 代谢对细胞色素 P450 3A4 和尿苷 5ʹ-二磷酸-葡萄糖醛酸基转移酶 1A1 的作用相似。在美国成人和青少年 HIV 治疗指南中，Bictegravir、dolutegravir 和 raltegravir 是大多数 HIV 感染者初始治疗方案的推荐成分。本综述总结并比较了整合酶链转移抑制剂药物的药代动力学和药效学，并描述了肝功能损害、肾功能不全、妊娠和合并感染患者的具体药代动力学注意事项。Bictegravir 代谢对细胞色素 P450 3A4 和尿苷 5ʹ-二磷酸-葡萄糖醛酸基转移酶 1A1 的作用相似。在美国成人和青少年 HIV 治疗指南中，Bictegravir、dolutegravir 和 raltegravir 是大多数 HIV 感染者初始治疗方案的推荐成分。本综述总结并比较了整合酶链转移抑制剂药物的药代动力学和药效学，并描述了肝功能损害、肾功能不全、妊娠和合并感染患者的具体药代动力学注意事项。