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Updated: Feb 13, 2026
05:23
Investigating Migraine-Like Behavior Using Light Aversion in Mice
Published on: August 11, 2021
4.5K
Targeted CGRP Small Molecule Antagonists for Acute Migraine Therapy
Philip R Holland1, Peter J Goadsby2
1Headache Group, Basic and Clinical Neuroscience, Institute of Psychiatry, Psychology and Neuroscience, King's College London, 125 Coldharbour Lane, London, UK. philip.holland@kcl.ac.uk.
Summary
Calcitonin gene-related peptide (CGRP) antagonists show promise for migraine treatment. While daily use raised safety concerns, intermittent administration and CGRP-targeted monoclonal antibodies offer effective and safe therapeutic options.
Area of Science:
- Neurology
- Pharmacology
Background:
- Migraine is a prevalent neurological disorder with significant unmet needs for acute therapies.
- Current treatments leave approximately 50% of patients dissatisfied.
- Calcitonin gene-related peptide (CGRP) is implicated in migraine pathophysiology.
Purpose of the Study:
- To review the development and clinical efficacy of CGRP receptor antagonists for migraine.
- To assess the safety and viability of CGRP-targeted therapies.
Main Methods:
- Review of clinical trial data for small molecule CGRP receptor antagonists.
- Evaluation of safety profiles, including liver toxicity concerns.
- Assessment of CGRP and CGRP receptor-targeted monoclonal antibodies.
Main Results:
- Small molecule CGRP receptor antagonists have demonstrated positive clinical trial results.
- Daily administration of some molecules led to liver toxicity and discontinuation.
- Intermittent use of CGRP antagonists appears viable and safe.
- CGRP-targeted monoclonal antibodies show good clinical efficacy.
Conclusions:
- CGRP is a validated target for migraine therapy.
- Intermittent use of small molecule CGRP antagonists and CGRP-targeted monoclonal antibodies represent promising therapeutic strategies for migraine management.
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