Department of Internal Medicine I, University of Bonn, Bonn, Germany.
Curr Opin HIV AIDS. 2012 Sep;7(5):456-62. doi: 10.1097/COH.0b013e328356e933.
To summarise recently published clinical studies of chemokine receptor-5 (CCR5)-blockers, including the small-molecule blocker, maraviroc (MVC) and CCR5-monoclonal antibodies for HIV. MVC may have immunomodulating properties through CCR5-blockade. MVC appears well tolerated and penetrates the central nervous system. For these reasons, MVC is being investigated in immunodiscordance, prevention of IRIS and in HCV-HIV co-infection. Novel techniques allow tropism assignment via sequencing of proviral DNA; this testing platform is being utilised in MVC switch studies in those with HIV viraemia below the level of quantification. MVC is being utilised in regimen intensification studies for HIV associated neurocognitive disease.
MVC has no anti-inflammatory activity in rheumatoid arthritis. MVC appears well tolerated in hepatitis virus co-infected patients and MVC-intensification in HCV-HIV co-infection suggests a favourable impact on liver fibrosis. Early pilot data suggests MVC intensification may have functional benefit in the CNS. There is a growing body of data on tropism testing using proviral DNA; this technology is being utilised in MVC switch studies. CCR5-monoclonal antibodies administered subcutaneously are promising in Phase II development.
The place of MVC as an anti-HIV drug in the switch setting and as an immunomodulator is yet to be fully determined.
总结最近发表的趋化因子受体 5（CCR5）-阻断剂的临床研究，包括小分子阻断剂马拉维若（MVC）和 CCR5-单克隆抗体治疗 HIV。MVC 通过阻断 CCR5 可能具有免疫调节特性。MVC 耐受性良好，可穿透中枢神经系统。基于这些原因，MVC 正在免疫失调、预防 IRIS 和 HCV-HIV 合并感染中进行研究。新的技术允许通过前病毒 DNA 测序进行趋性分配；该检测平台正在用于 MVC 转换研究中 HIV 病毒血症低于检测下限的患者。MVC 正在用于治疗 HIV 相关神经认知疾病的强化方案研究中。
MVC 在类风湿关节炎中没有抗炎活性。MVC 在合并肝炎病毒感染的患者中耐受性良好，在 HCV-HIV 合并感染中加强 MVC 治疗提示对肝纤维化有有利影响。早期的初步数据表明，MVC 强化治疗可能对中枢神经系统有功能益处。越来越多的数据使用前病毒 DNA 进行趋性检测；这项技术正在用于 MVC 转换研究。皮下给予 CCR5-单克隆抗体具有良好的发展前景。
MVC 作为一种 HIV 药物在转换治疗中的地位和作为免疫调节剂的地位尚未完全确定。
