Calcitonin gene-related peptide (CGRP) is a neuropeptide involved in vasodilation and cerebrovascular regulation. CGRP is the most potent vasoactive constituent of the trigeminovascular system and has a key role in migraine. CGRP-targeted medications represent a new class of migraine-specific therapies. CGRP receptor antagonists, termed “gepants,” are selective, oral, and small molecule medications developed for both the acute and preventive migraine treatments. Currently, rimegepant, ubrogepant, and zavegepant are approved for the acute treatment of migraine in adults. Several key clinical trials have demonstrated their efficacy and tolerability as compared to placebo. The ongoing development of real-world evidence and long-term safety data will help determine the role of gepants in the current migraine treatment landscape.