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Papers of the Week

Papers: 29 May 2021 - 4 Jun 2021

Pharmacology/Drug Development


2021 Jun 02

Br J Pharmacol

CGRP receptor antagonists for migraine – are they also AMY receptor antagonists?


Garelja ML, Walker CS, Hay DL
Br J Pharmacol. 2021 Jun 02.
PMID: 34076887.


The development of several drugs that target the calcitonin gene-related peptide (CGRP) system has been a major breakthrough in the pharmacological management of migraine. These are divided into two major classes: antibodies which bind to the CGRP peptide, preventing it from activating CGRP receptors and receptor antagonists. Within the receptor antagonist class, there are two mechanisms of action: small molecule receptor antagonists and an antibody antagonist. This mini-review considers the pharmacology of these receptor targeted antagonist drugs at the CGRP receptor and closely-related AMY receptor, at which CGRP may also act. The antagonists are most potent at the CGRP receptor but can also show antagonism of the AMY receptor. However, important data are missing and selectivity parameters cannot be provided for all antagonists. The clinical implications of AMY receptor antagonism are unknown but we urge consideration of this receptor as a potential contributing factor to CGRP and antagonist drug actions.