Calcitonin gene-related peptide receptor antagonist


Calcitonin gene-related peptide receptor antagonists are a class of drug candidates that act as antagonists of the calcitonin gene-related peptide receptor.
CGRPR antagonists are under investigation as potential antimigraine agents and also in the context of osteoarthritis.

Examples

Non-peptide small molecules

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.

Migraine

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.

Metabolic health

Mice given a CGRP receptor antagonist improved insulin secretion and reduced chronic inflammation, improving the metabolic health of the animals.