CGRP受体拮抗剂治疗偏头痛的研究进展

Research Progress in Treatment of Migraine with CGRP Receptor Antagonists

偏头痛是一种十分普遍的神经系统疾病,对社会和患者的日常生活有极大影响。降钙素基因相关肽(CGRP)是一种在偏头痛发生过程中起重要作用的神经递质。通过阻断CGRP或其受体可治疗和预防偏头痛发作,由此开发的药物包括小分子CGRP受体拮抗剂和CGRP单克隆抗体。早期的CGRP受体拮抗剂由于生物利用度低、肝毒性等已终止研究。目前,Rimegepant、Vazegepant、Ubrogepant、Atogepant四种CGRP受体拮抗剂在治疗偏头痛的临床试验中显示出良好的疗效和耐受性,其中Rimegepant和Ubrogepant已被美国食品药品管理局批准用于临床。未来还需要深入研究CGRP受体拮抗剂,以期更好地应用于偏头痛的治疗。

Migraine is a very common nervous system disease,which has a great impact on the society and the daily life of patients.Calcitonin gene-related peptide(CGRP)is a neurotransmitter that plays an important role in migraine.Drugs developed to treat and prevent migraine attacks by blocking CGRP or its receptor include small-molecule CGRP receptor antagonists and CGRP monoclonal antibodies.Early studies on CGRP receptor antagonists have been terminated due to low bioavailability,hepatotoxicity and other reasons.At present,Rimegepant,Vazegepant,Ubrogepant and Atogepant,four CGRP receptor antagonists,have shown good efficacy and tolerability in the clinical trials of the treatment of migraine,among which Rimegepant and Ubrogepant have been approved by the U.S.Food and Drug Administration for clinical application.Further research on CGRP receptor antagonists is needed in the future for better application in the treatment of migraine.