Tso Amy R, Goadsby Peter J
Basic and Clinical Neuroscience, Institute of Psychiatry, Psychology and Neuroscience, King's College London, London, UK.
NIHR-Wellcome Trust King's Clinical Research Facility, King's College Hospital, Wellcome Foundation Building, London, SE5 9PJ, UK.
Curr Treat Options Neurol. 2017 Aug;19(8):27. doi: 10.1007/s11940-017-0463-4.
Migraine is a very disabling disorder with severe impact on patients' lives and substantive costs to society in terms of healthcare costs and lost productivity. Prevention is a key component of migraine therapy, and while numerous preventive options exist, each is burdened by either troublesome side effects or insufficient efficacy. All migraine preventives currently in clinical use were licensed for other purposes and, by chance, have efficacy against migraine. As our understanding of migraine has evolved, calcitonin gene-related peptide (CGRP) has moved to the forefront as a neuropeptide central to migraine pathophysiology. Six small molecule CGRP receptor antagonists were shown to be effective for acute treatment of migraine; two were stopped for hepatotoxicity or one for formulation concern issues and one is now in phase III. Monoclonal antibodies against CGRP or the CGRP receptor have a longer duration of action and have been investigated for migraine prevention. Four are in development and three have completed phase II and one phase III trials; every reported study has been positive. Furthermore, no safety issues have arisen to date, including hepatic or cardiovascular effects, and initial tolerability appears to be excellent. Monoclonal antibodies antagonizing the CGRP pathway represent a novel approach to prevention: a mechanism-specific migraine-targeted therapy. While we must await the results of all the phase III trials, cautious excitement seems warranted as we enter a new era of better tolerated, well-understood, bespoke migraine treatment for this common and disabling neurological disorder.
偏头痛是一种极具致残性的疾病,对患者的生活造成严重影响,并在医疗费用和生产力损失方面给社会带来巨大成本。预防是偏头痛治疗的关键组成部分,虽然有多种预防选择,但每种方法都存在令人烦恼的副作用或疗效不足的问题。目前临床使用的所有偏头痛预防药物最初都是为其他目的获批的,只是偶然发现对偏头痛有效。随着我们对偏头痛认识的不断发展,降钙素基因相关肽(CGRP)作为偏头痛病理生理学的核心神经肽已成为研究重点。六种小分子CGRP受体拮抗剂已被证明对偏头痛急性治疗有效;其中两种因肝毒性被停用,一种因制剂相关问题被停用,还有一种目前处于III期试验阶段。抗CGRP或CGRP受体的单克隆抗体作用时间更长,已被研究用于偏头痛预防。四种处于研发阶段,三种已完成II期试验,一种已完成III期试验;每项报告的研究结果均为阳性。此外,迄今为止尚未出现包括肝脏或心血管影响在内的安全问题,初步耐受性似乎良好。拮抗CGRP途径的单克隆抗体代表了一种新的预防方法:一种针对偏头痛机制的特异性治疗。虽然我们必须等待所有III期试验的结果,但随着我们进入一个针对这种常见且致残的神经系统疾病的耐受性更好、理解更深入、定制化的偏头痛治疗新时代,谨慎的兴奋似乎是有道理的。