Makinson Alain, Reynes Jacques
Infectious Diseases Department, Montpellier University Hospital, CHU Montpellier, France.
Curr Opin HIV AIDS. 2009 Mar;4(2):150-8. doi: 10.1097/COH.0b013e32832498d8.
The purpose of this review is to discuss recent pharmacological, virological, and clinical data that concern enfuvirtide usage in different antiretroviral combinations.
Randomized, recent trials in multidrug-experienced patients suggest that antiretroviral combinations with enfuvirtide have excellent virological responses with new antiretroviral compounds, including darunavir, etravirine, raltegravir, vicriviroc, and maraviroc. Trials confirm long-term safety, in spite of moderate injection-site reactions or pain, and lack of significant interactions. Preliminary data suggest that switching from enfuvirtide to raltegravir is effective and using enfuvirtide in prophylaxis of mother-to-child transmission is well tolerated. To administer enfuvirtide in an intensification strategy in antiretroviral-naïve or experienced populations may accelerate virological decline.
Dosage adaptations to renal insufficiency are not necessary with enfuvirtide. Spinal fluid concentrations and ombilic cord passage are negligible. Durability of virological responses with enfuvirtide in combinations has been confirmed, in spite of injection-site reactions and twice daily subcutaneous administration. Enfuvirtide should be used with at least one other fully active drug in optimized background therapy in multidrug-experienced populations, a possible exception being with entry inhibitors, which may further benefit from the addition of a third active drug. Data concerning enfuvirtide in antiretroviral combinations show accelerated viral load decline, and the possibility of switching from enfuvirtide to raltegravir without modification of optimized background therapy.
本综述旨在讨论近期有关恩夫韦肽在不同抗逆转录病毒联合用药中的药理学、病毒学及临床数据。
针对有多种药物治疗经验患者的随机近期试验表明，含恩夫韦肽的抗逆转录病毒联合用药与包括达芦那韦、依曲韦林、拉替拉韦、维立西呱和马拉维若在内的新型抗逆转录病毒化合物联用，具有出色的病毒学应答。试验证实了其长期安全性，尽管存在中度注射部位反应或疼痛，且无显著相互作用。初步数据表明，从恩夫韦肽转换为拉替拉韦是有效的，且恩夫韦肽用于预防母婴传播耐受性良好。在初治或有治疗经验的人群中采用强化策略使用恩夫韦肽可能会加速病毒学下降。
恩夫韦肽无需根据肾功能不全调整剂量。脑脊液浓度和脐带通过率可忽略不计。尽管存在注射部位反应且需每日皮下注射两次，但含恩夫韦肽联合用药的病毒学应答持久性已得到证实。在有多种药物治疗经验的人群中，恩夫韦肽应与至少一种其他完全有效的药物联合用于优化背景治疗，进入抑制剂可能是个例外，其可能会从添加第三种活性药物中进一步获益。有关恩夫韦肽在抗逆转录病毒联合用药中的数据显示病毒载量下降加速，且在不改变优化背景治疗的情况下从恩夫韦肽转换为拉替拉韦是可行的。
