Clinical Unit of Infectious Diseases, Microbiology, and Preventive Medicine, HIV and PK Research Group, Institute of Biomedicine of Seville (IBiS), University of Seville, CSIC, University Hospital Virgen del Rocío, Sevilla, Spain.
AIDS Rev. 2017 Oct-Dec;19(3):156-166.
During the past 30 years of antiretroviral therapy, continuous improvements in drug discovery have provided increasingly potent and safer antivirals that have transformed HIV infection in a chronic illness, rarely fatal. Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are frequently used as part of any antiretroviral combination therapy. Side effects and low resistance barrier of fi rst-generation NNRTIs (e.g., nevirapine and efavirenz) have been overcome with rilpivirine (RPV), and the last NNRTI approved for the treatment of HIV infection. The good efficacy, safety profi le, and convenient dosing of RPV account for the unique durability of RPV-based regimens. The advent of new oral fi xed-dose coformulations of RPV (e.g., along with dolutegravir or with tenofovir alafenamide [TAF]/emtricitabine [FTC]) as well as the development of long-acting injectable RPV nanoformulations will further expand its therapeutic landscape, including RPV use in dual maintenance therapy in HIV-infected patients or as pre-exposure prophylaxis in high-risk uninfected individuals.
在过去 30 年的抗逆转录病毒治疗中，药物发现的不断改进提供了越来越有效和更安全的抗病毒药物，将 HIV 感染转变为慢性疾病，很少致命。非核苷类逆转录酶抑制剂（NNRTIs）经常作为任何抗逆转录病毒联合治疗方案的一部分使用。第一代 NNRTIs（如奈韦拉平、依法韦仑）的副作用和低耐药屏障已经被利匹韦林（RPV）克服，它是最后一种被批准用于治疗 HIV 感染的 NNRTI。RPV 的良好疗效、安全性和方便的给药剂量是 RPV 为基础的治疗方案独特的持久性的原因。新的 RPV 固定剂量复方制剂（例如与多替拉韦或与替诺福韦艾拉酚胺[TAF]/恩曲他滨[FTC]）的出现以及长效注射 RPV 纳米制剂的开发将进一步扩大其治疗范围，包括在 HIV 感染患者的双重维持治疗中使用 RPV 或在高风险未感染个体中作为暴露前预防。
