Department of Human Neurosciences, Sapienza University of Rome , Rome, Italy.
International Mood & Psychotic Disorders Research Consortium, Mailman Research Center, McLean Hospital , Belmont, Massachusetts, USA.
Expert Opin Pharmacother. 2020 May;21(7):755-759. doi: 10.1080/14656566.2020.1721462. Epub 2020 Feb 3.
Migraine is a neurovascular disorder involving neurogenic inflammation and transmission of trigeminovascular nociceptive pathways mediated by Calcitonin Gene-Related Peptide (CGRP). Several small molecules antagonizing the CGRP receptor have been developed as migraine-specific acute medications. The CGRP receptor antagonist ubrogepant, also known as MK-1602, has been recently evaluated in phase III clinical trials for clinical efficacy and long-term safety as an abortive migraine treatment.
This paper discusses the pharmacodynamics, pharmacokinetics, clinical efficacy, safety, and tolerability profile of ubrogepant for the acute treatment of migraine with or without aura.
Ubrogepant, a selective CGRP antagonist belonging to the gepants family, has been evaluated in large short- and long-term Phases 2 and 3 clinical trials aimed to assess clinical efficacy and safety as acute migraine medication. It did not significantly affect liver function and was not associated with other serious adverse events. Long-term non-serious adverse events were similar between placebo and ubrogepant. The efficacy was evaluated in large placebo-controlled studies and ubrogepant 50 mg and 100 mg was superior, even if the therapeutic gain seems to be low. Nevertheless, the favorable safety profile compared to other abortive drugs makes ubrogepant a promising option for the acute treatment of migraine.
偏头痛是一种涉及神经源性炎症和降钙素基因相关肽(CGRP)介导的三叉神经血管伤害性通路传递的神经血管疾病。已经开发出几种拮抗 CGRP 受体的小分子,作为偏头痛特异性急性药物。CGRP 受体拮抗剂ubrogepant,也称为 MK-1602,最近在 III 期临床试验中评估了其作为偏头痛急性治疗的临床疗效和长期安全性。
本文讨论了ubrogepant 作为一种急性偏头痛治疗药物的药效学、药代动力学、临床疗效、安全性和耐受性特征,包括有无先兆的偏头痛。
Ubrogepant 是一种属于 gepants 家族的选择性 CGRP 拮抗剂,已经在大型短期和长期的 II 期和 III 期临床试验中进行了评估,旨在评估其作为急性偏头痛药物的临床疗效和安全性。它对肝功能没有显著影响,也没有与其他严重不良事件相关。安慰剂和 ubrogepant 之间的长期非严重不良事件相似。在大型安慰剂对照研究中评估了疗效,ubrogepant 50mg 和 100mg 更为有效,尽管治疗效果似乎较低。然而,与其他偏头痛急性治疗药物相比,其良好的安全性特征使 ubrogepant 成为一种有前途的选择。