Peytavin Gilles, Calvez Vincent, Katlama Christine
Laboratoire de Toxicologie et Pharmacocinétique, Centre Hospitalier Universitaire Xavier Bichat-Claude Bernard, Paris, France.
Therapie. 2009 Jan-Feb;64(1):9-16. doi: 10.2515/therapie/2009006. Epub 2009 May 26.
A decade after identification of the chemokine receptor CCR5 as a coreceptor for human immunodeficiency virus (HIV), the first CCR5 antagonist has recently been approved by the European Medicines Evaluation Agency (EMEA) for treatment of HIV infected patients. Maraviroc (Celsentri is a small molecule that specifically inhibits CCR5 and thereby blocks HIV entry into its target cells. Viral tropism testing is mandatory before prescribing maraviroc, due to its unique mode of action limited to CCR5-tropic viruses. Maraviroc is administered orally, twice daily. Daily dose must be adapted in case of association with a cytochrome P450 inducer or inhibitor. Efficacy of maraviroc has been demonstrated in patients failing other antiretroviral classes. Its potential for first line or switch therapy has to be proven in future trials.
在趋化因子受体CCR5被确定为人类免疫缺陷病毒(HIV)的共受体十年后,首个CCR5拮抗剂最近已获欧洲药品评估局(EMEA)批准用于治疗HIV感染患者。马拉维若(Celsentri)是一种小分子,可特异性抑制CCR5,从而阻止HIV进入其靶细胞。由于其独特的作用方式仅限于亲嗜CCR5的病毒,因此在开处方使用马拉维若之前必须进行病毒嗜性检测。马拉维若口服给药,每日两次。如果与细胞色素P450诱导剂或抑制剂联合使用,必须调整每日剂量。马拉维若在其他抗逆转录病毒药物治疗失败的患者中已显示出疗效。其用于一线治疗或换药治疗的潜力还有待在未来试验中得到证实。