Cohen Fred, Yuan Hsiangkuo
Jefferson Headache Center, Department of Neurology, Thomas Jefferson University, Philadelphia, PA, 19107, USA.
Ther Clin Risk Manag. 2022 Apr 22;18:447-456. doi: 10.2147/TCRM.S348724. eCollection 2022.
Advances in molecular biology and neuroscience have led to the discovery of calcitonin gene-related peptide (CGRP), a 37 amino-acid neuropeptide that plays a critical role in the pathogenesis of migraine. CGRP receptor antagonist, also known as gepant, is an oral medication that inhibits the CGRP-related nociceptive signaling pathway. To date, three gepants are approved by the FDA for migraine treatment. Atogepant is a 2nd-generation gepant that non-competitively antagonizes CGRP receptors inhibiting neurogenic inflammation and pain sensitization. With its long half-life and minimal cardiovascular or liver toxicity, it is the first in its class approved primarily for migraine prevention. This article will discuss the evidence, safety, and rationale of atogepant for use in clinical practice.
分子生物学和神经科学的进展促使人们发现了降钙素基因相关肽(CGRP),这是一种由37个氨基酸组成的神经肽,在偏头痛的发病机制中起关键作用。CGRP受体拮抗剂,也称为gepant,是一种口服药物,可抑制与CGRP相关的伤害性信号通路。迄今为止,有三种gepant已获美国食品药品监督管理局(FDA)批准用于偏头痛治疗。阿托格潘是第二代gepant,它非竞争性地拮抗CGRP受体,抑制神经源性炎症和疼痛敏化。由于其半衰期长且心血管或肝脏毒性极小,它是同类药物中首个主要获批用于偏头痛预防的药物。本文将讨论阿托格潘在临床实践中应用的证据、安全性及理论依据。