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CGRP inhibitors

Written by C. Fookes, BPharm on Nov 7, 2018

Other names: calcitonin gene-related peptide inhibitors

What are CGRP inhibitors?

Calcitonin gene-related peptide (CGRP) inhibitors block the effect of CGRP, which is a small protein that is highly prevalent in the sensory nerves that supply the head and the neck. CGRP is involved in pain transmission and levels increase during a migraine attack. It may also play a causative role in the induction of migraine attacks. CGRP inhibitors are used for the management of migraine.

There are two types of CGRP inhibitors – monoclonal antibodies and CGRP receptor antagonists (gepants).

Monoclonal antibodies target either CGRP or the CGRP receptor and are used for migraine prevention. A monoclonal antibody is a collection of identical proteins that have been developed to only target one substance in the body. They are given by injection subcutaneously (under the skin), to avoid degradation by the stomach. Because they are large molecules, they take longer to start working and work in the lining of the brain rather than in the brain itself. They also tend to have few drug interactions and are unlikely to cause liver or kidney damage. Currently, three CGRP inhibitors that are monoclonal antibodies have been approved:

  • Aimovig (erenumab-aooe): Approved May 17, 2018
  • Ajovy (fremanezumab): Approved Sept 14, 2018
  • Emgality (galcanezumab-gnlm): Approved Sept 27, 2018
  • Eptinezumab: Not yet approved.

Gepants are small molecule drugs which block the CGRP receptor and are still being investigated for both migraine relief and prevention. Unlike monoclonal antibodies, gepants rapidly penetrate the brain so work quickly; however, they are metabolized in the liver so there is a higher potential for interactions and possibly liver damage. Examples include ubrogepant, atogepant, and rimegepant.

CGRP inhibitors are the first drugs to be developed specifically for migraine prevention. All other migraine preventive agents were originally developed for other conditions (such as high blood pressure), and then found later by chance to have an effect in migraine.

List of CGRP inhibitors:

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Drug Name Reviews Avg. Ratings
Ajovy (Pro)
Generic name: fremanezumab
42 reviews
Aimovig (Pro)
Generic name: erenumab
375 reviews
Emgality (Pro)
Generic name: galcanezumab
101 reviews

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

See Also

Medical conditions associated with CGRP inhibitors: