St Stephen's Centre, Chelsea and Westminster Hospital and Foundation Trust.
Department of Medicine, Imperial College London, London, UK.
Curr Opin HIV AIDS. 2018 Jul;13(4):300-307. doi: 10.1097/COH.0000000000000474.
Rilpivirine is a non-nucleoside reverse transcriptase inhibitor approved for the treatment of HIV in combination with other antiretrovirals (ARV). The development of the long-acting formulation of rilpivirine (RPV-LA) and its use in clinical settings is the subject of this review.
In 2017, the results of the phase IIb study LATTE2 have been published. This study demonstrated that the combination of RPV-LA with a second long-acting agent (cabotegravir) administered intramuscularly every 4--8 weeks was similar in virologic suppression rates to standard of care ARV treatment.
RPV-LA is an injectable nanoparticle suspension for intramuscular use. Phase I studies in healthy volunteers demonstrated that RPV-LA, administered at doses between 600 and 1200 mg, was well tolerated and effective in maintaining satisfactory drug concentrations in plasma, vaginal secretions and rectal tissue compartments for at least 4 weeks. RPV-LA efficacy was also shown in a phase II clinical trial in HIV infected patients and phase III studies are currently ongoing. Most study participants stated that they would use or continue using injectables, both in HIV treatment and prevention settings. Long-acting injectable ARVs have the potential to improve the convenience of HIV drug regimens.
利匹韦林是一种非核苷类逆转录酶抑制剂，与其他抗逆转录病毒药物（ARV）联合用于治疗 HIV。本文对利匹韦林长效制剂（RPV-LA）的研发及其在临床应用的相关研究进展进行综述。
2017 年，发表了 IIb 期 LATTE2 研究的结果。该研究表明，RPV-LA 联合第二种长效制剂（卡替拉韦）每 4-8 周肌内注射的方案，在病毒抑制率方面与标准的 ARV 治疗相当。
RPV-LA 是一种用于肌内注射的纳米颗粒混悬剂。在健康志愿者中进行的 I 期研究表明，RPV-LA 在 600-1200mg 剂量范围内，具有良好的耐受性，能有效维持至少 4 周的血浆、阴道分泌物和直肠组织中令人满意的药物浓度。在 HIV 感染患者中进行的 II 期临床试验和 III 期研究也证实了 RPV-LA 的疗效。大多数研究参与者表示，他们愿意或会继续在 HIV 治疗和预防环境中使用注射剂。长效注射型 ARV 有可能提高 HIV 药物治疗方案的便利性。
