Calcitonin gene-related peptide receptor antagonist
Class of drugs
Class of drugs
Calcitonin gene-related peptide (CGRP) receptor antagonists, commonly known as gepants, are a class of drugs that act as antagonists of the calcitonin gene-related peptide receptor (CGRPR). The CGRP family of small proteins are present in the sensory nerves of the head and neck and are involved in transmission of pain. Nerve activation can trigger the release of CGRP and other neuropeptides, leading to inflammation, pain, and swelling in the case of migraine. Several monoclonal antibodies that bind to the CGRP receptor or peptide have been approved for prevention of migraine. As of March 11, 2024, the American Headache Society issued a statement that "CGRP targeting therapies are a first-line option for migraine prevention" in the United States. The prior use of non-specific migraine preventive medication approaches is therefore no longer required before CGRP treatments can be prescribed. CGRP inhibitors are significantly more expensive on an annual basis than most of the older therapies...
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