Calcitonin gene-related peptide (CGRP) receptor antagonists are a class of drugs that act as
antagonist
An antagonist is a character in a story who is presented as the chief foe of the protagonist.
Etymology
The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...
s of the
calcitonin gene-related peptide receptor (CGRPR).
Several
monoclonal antibodies
A monoclonal antibody (mAb, more rarely called moAb) is an antibody produced from a cell Lineage made by cloning a unique white blood cell. All subsequent antibodies derived this way trace back to a unique parent cell.
Monoclonal antibodies ca ...
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 agent
Antimigraine drugs are medications intended to reduce the effects or intensity of migraine headache. They include drugs for the treatment of acute migraine symptoms as well as drugs for the prevention of migraine attacks.
Treatment of acute symp ...
s.
Drugs of this class have also been investigated for use in
osteoarthritis.
Examples
Non-peptide small molecules
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Ubrogepant is approved for acute treatment of migraines
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Rimegepant
Rimegepant, sold under the brand name Nurtec ODT among others, is a medication used for the acute treatment of migraine with or without aura in adults and the preventative treatment of episodic migraine in adults. It is taken by mouth to diss ...
(BMS-927711) is approved for acute and preventative treatment of migraines
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Atogepant (AGN-241689) is approved for preventative treatment of migraines
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Telcagepant
Telcagepant (INN) (code name MK-0974) is a calcitonin gene-related peptide receptor antagonist which was an investigational drug for the acute treatment and prevention of migraine, developed by Merck & Co.
In the acute treatment of migraine, ...
(MK-0974), reached phase III clinical trials; development discontinued in 2011.
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Olcegepant
Olcegepant (INN
Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also ...
(BIBN-4096BS) is a drug candidate
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BI 44370 TA (BI 44370)
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MK-3207
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SB-268262
Monoclonal antibodies targeting the CGRP receptor
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Erenumab (AMG-334) is approved for prevention of migraine.
Monoclonal antibodies targeting the CGRP molecule
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Eptinezumab (ALD403) is approved for prevention of migraine.
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Fremanezumab (TEV-48125) is approved for prevention of migraine.
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Galcanezumab (LY2951742) is approved for prevention of migraine and
cluster headaches.
Necrotizing fasciitis
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.
As of February 2020, Vyepti (
eptinezumab) was FDA approved for the treatment of migraine via intravenous infusion as well.
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.
Metabolic health
Mice given a CGRP receptor antagonist improved insulin secretion and reduced chronic inflammation, improving the metabolic health of the animals.
References
Antimigraine drugs
Receptor antagonists
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