Department of Neurology, Mayo Clinic, Scottsdale, AZ, United States.
Department of Neurology, Mayo Clinic, Scottsdale, AZ, United States.
Prog Brain Res. 2020;255:143-170. doi: 10.1016/bs.pbr.2020.06.019. Epub 2020 Jul 22.
Calcitonin Gene-Related Peptide (CGRP) plays a pivotal role in migraine pathophysiology. Two types of CGRP function-blocking modalities, monoclonal antibodies, and small molecules (gepants), have been developed to target the CGRP ligands and CGRP receptors. Four CGRP monoclonal antibodies have received FDA approval for the prevention of migraine: erenumab, fremanezumab, galcanezumab, and eptinezumab. Two gepants have been approved by the FDA for the acute treatment of migraine: ubrogepant and rimegepant. Multiple clinical trials of the CGRP monoclonal antibodies and gepants, and now some open-label long-term extension data, established their efficacy, safety, and tolerability. In this chapter, we summarize the major clinical trials, pharmacokinetic insights, safety and tolerability profiles, and real-world data (if available) of the CGRP monoclonal antibodies and gepants.
降钙素基因相关肽(CGRP)在偏头痛发病机制中起着关键作用。已经开发出两种 CGRP 功能阻断方式,即单克隆抗体和小分子( gepants),以靶向 CGRP 配体和 CGRP 受体。四种 CGRP 单克隆抗体已获得 FDA 批准用于预防偏头痛:erenumab、fremanezumab、galcanezumab 和 eptinezumab。两种 gepants 已获得 FDA 批准用于偏头痛的急性治疗:ubrogepant 和 rimegepant。CGRP 单克隆抗体和 gepants 的多项临床试验,以及现在的一些开放标签长期扩展数据,确立了它们的疗效、安全性和耐受性。在这一章中,我们总结了 CGRP 单克隆抗体和 gepants 的主要临床试验、药代动力学见解、安全性和耐受性概况以及真实世界数据(如果有)。