Calcitonin gene-related peptide receptor antagonist
Several monoclonal antibodies which binds to the CGRP receptor or peptide have been approved for prevention of migraine. Three small molecule CGRPR antagonists are approved in the U.S. as antimigraine agents. Drugs of this class have also been investigated for use in osteoarthritis.
Non-peptide small molecules
- Ubrogepant is approved for acute treatment of migraines
- Rimegepant (BMS-927711) is approved for acute and preventative treatment of migraines
- Atogepant (AGN-241689) is approved for preventative treatment of migraines
- Telcagepant (MK-0974), reached phase III clinical trials; development discontinued in 2011.
- Olcegepant (BIBN-4096BS) is a drug candidate
- BI 44370 TA (BI 44370)
Monoclonal antibodies targeting the CGRP receptor
Monoclonal antibodies targeting the CGRP molecule
- Eptinezumab (ALD403) is approved for prevention of migraine.
- Fremanezumab (TEV-48125) is approved for prevention of migraine.
- Galcanezumab (LY2951742) is approved for prevention of migraine and cluster headaches.
A study has found botox effective against necrotizing fasciitis caused by S. pyogenes in mice. 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. Botox blocks the CGRP cascade of nerve cells.
As of 2018, erenumab, trade name Aimovig, was approved in the U.S. for use for migraines. It interacts by blocking the CGRP receptor. As of 2018, fremanezumab, trade name Ajovy, was approved in the U.S. for use for migraines. It interacts with the CGRP protein expressed during an attack. The third approved treatment, as of 2018, galcanezumab, trade name Emgality, was approved in the U.S. for use in migraines. It also interacts with the protein.
Three small-molecule antagonists have been approved for treatment of migraine: ubrogepant, rimegepant, and atogepant. Ubrogepant and rimegepant are approved for acute treatment. Atogepant and rimegepant are approved for preventative treatment.
Mice given a CGRP receptor antagonist improved insulin secretion and reduced chronic inflammation, improving the metabolic health of the animals.
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