AI Article Synopsis
- Small molecule CGRP receptor antagonists, known as gepants, emerged as a potential treatment for migraines between 2004 and 2011, but initial development faced challenges like oral availability and liver toxicity concerns.
- The newer generation of gepants, including ubrogepant and rimegepant, has recently been approved for treating acute migraines, following a 15-year gap in development.
- The chapter reviews the effectiveness, safety, and tolerability of gepants, as well as their limitations and future potential in migraine treatment.
Article Abstract
Small molecule calcitonin gene-related peptide (CGRP) receptor antagonists are commonly referred to as gepants. The first generation of gepants provided the first line of evidence of CGRP-mediated antimigraine medication in 2004-2011. However, further development was halted due to either lack of oral availability or concerns of hepatotoxicity. More than 15 years later, the first second generation of gepants, ubrogepant and rimegepant, are now approved for the acute treatment of migraine with or without aura. Furthermore, a novel and promising third-generation gepant, zavegepant, has recently been approved as well. In this chapter, we review the evidence supporting the effectiveness, safety, and tolerability of gepants for the acute treatment of migraine. Furthermore, we discuss the potential limitations and future directions of this class of migraine-specific medication.
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| http://dx.doi.org/10.1016/B978-0-12-823357-3.00033-1 | DOI Listing |
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