不宁腿综合征为临床常见中枢神经系统感觉运动障碍性疾病,发病机制尚不明确,可能与遗传因素或多巴胺能系统功能失调有关。加巴喷丁恩那卡比最初由美国XenoPort公司研发,之后由英国葛兰素史克公司通过并购获得,临床试验验证了其治疗不宁腿综合征的有效性。综述了加巴喷丁恩那卡比的研发背景、合成方法、药理学、药动学、临床评价、安全性和耐受性等研究进展,以期为临床上更好地应用提供依据。

Restless legs syndrome (RLS) is a common clinical sensorimotor nervous system disorders. Its pathogenesis is uncertain and may be related to genetic factors or dopaminergic system dysfunction. Gabapentin enacarbil originally developed by the US company XenoPort, later was obtained by British GlaxoSmithKline through acquisitions, and clinical trials show the effectiveness of the treatment of RLS. This paper reviewed the research background, synthesis methods, pharmacology, pharmacokinetics, clinical evaluation, safety and tolerability of gabapentin enacarbil and provide the basis for better application in clinic.