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]

• Ubrogepant is approved for acute treatment of migraines ^{[7] [4]}
• Rimegepant (BMS-927711) is approved for acute and preventative treatment of migraines ^{[8] [3]}
• Atogepant (AGN-241689) is approved for preventative treatment of migraines ^[5]
• Zavegepant (BHV- 3500) is a nasal spray approved for acute treatment of migraines. ^{[9] [10]}
• Telcagepant (MK-0974), reached phase III clinical trials; development discontinued in 2011. ^[11]
• Olcegepant (BIBN-4096BS) is a drug candidate ^[12]
• BI 44370 TA (BI 44370) ^[13]
• MK-3207 ^[14]
• SB-268262

• Erenumab (AMG-334) is approved for prevention of migraine. ^[15]

• Eptinezumab (ALD403) is approved for prevention of migraine. ^[16]
• Fremanezumab (TEV-48125) is approved for prevention of migraine. ^{[17] [18]}
• Galcanezumab (LY2951742) is approved for prevention of migraine and cluster headaches. ^[19]

A study has found botox effective against necrotizing fasciitis caused by S. pyogenes in mice. ^[20] Its mechanism of action is by blocking CGRP receptor of nerve cells, which trigger intense pain and activate CGRP cascade, which prevents the immune system attacks to control the pathogen. ^[21] Botox blocks the CGRP cascade of nerve cells. ^[22]

As of 2018, erenumab, brand name Aimovig, was approved in the U.S. for use for migraines. It interacts by blocking the CGRP receptor. ^[23] As of 2018, fremanezumab, brand name Ajovy, was approved in the U.S. for use for migraines. It interacts with the CGRP protein expressed during an attack. ^[24] The third approved treatment, as of 2018, galcanezumab, brand name Emgality, was approved in the U.S. for use in migraines. It also interacts with the protein. ^[25]

As of February 2020, eptinezumab (Vyepti) was approved by the FDA for the treatment of migraine via intravenous infusion as well. ^[26]

Three small-molecule antagonists have been approved for treatment of migraine: ubrogepant, rimegepant, and atogepant. ^{[4] [3] [5]} Ubrogepant and rimegepant are approved for acute treatment. ^{[4] [3]} Atogepant and rimegepant are approved for preventative treatment. ^{[5] [3]}