Calcitonin gene-related peptide (CGRP) receptor antagonists are a class of drugs that act as antagonists of the calcitonin gene-related peptide receptor (CGRPR).[1]
Several monoclonal antibodies that bind to the CGRP receptor or peptide have been approved for prevention of migraine.[2]Nerve activation triggers the release of CGRP and other neuropeptides, leading to inflammation, pain, and swelling. Three small molecule CGRPR antagonists are approved in the U.S. as antimigraine agents.[3][4][5] Drugs of this class have also been investigated for use in osteoarthritis.[6]
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