Gepants
(2025) p.295-304- Abstract
Calcitonin gene-related peptide (CGRP) was suggested to play an important role in primary headaches as far back as 1985 and has been confirmed as playing a significant role in migraine pathophysiology. CGRP receptor antagonists are becoming more and more important for treatment of acute migraine attacks and for prophylaxis of episodic and chronic migraine. The development of drugs that bind CGRP or its canonical receptor are monoclonal antibodies for prophylaxis and small molecular gepants, that block the receptor, acting both in acute attacks of migraine and in prophylaxis. They have all been shown to relieve migraine pain in clinical trials, and their molecular mechanisms involve binding and inhibiting CGRP receptors in the... (More)
Calcitonin gene-related peptide (CGRP) was suggested to play an important role in primary headaches as far back as 1985 and has been confirmed as playing a significant role in migraine pathophysiology. CGRP receptor antagonists are becoming more and more important for treatment of acute migraine attacks and for prophylaxis of episodic and chronic migraine. The development of drugs that bind CGRP or its canonical receptor are monoclonal antibodies for prophylaxis and small molecular gepants, that block the receptor, acting both in acute attacks of migraine and in prophylaxis. They have all been shown to relieve migraine pain in clinical trials, and their molecular mechanisms involve binding and inhibiting CGRP receptors in the trigeminovascular system. The current view on migraine pathology suggests that binding CGRP receptors on the Aδ-neurons is the main molecular site by which they exhibit their beneficial effects. Here the background to the small molecular gepants is provided and followed by description of the recent phase III data on the second generation of gepants designed for use in acute attacks: ubrogepant, rimegepant and zavegepant. They have all been found effective with minor side-effects and can safely be combined with previously approved medications which provide the patients with novel ways to alleviate their migraine.
(Less)
- author
- Edvinsson, Lars LU
- organization
- publishing date
- 2025
- type
- Chapter in Book/Report/Conference proceeding
- publication status
- published
- subject
- keywords
- CGRP, CGRP receptor, Gepant, Migraine, Pathophysiology, Trigeminovascular system
- host publication
- Migraine Pain Management : Current Pharmacological and Non-pharmacological Options - Current Pharmacological and Non-pharmacological Options
- pages
- 10 pages
- publisher
- Elsevier
- external identifiers
-
- scopus:85213191290
- ISBN
- 9780443247057
- 9780443247040
- DOI
- 10.1016/B978-0-443-24705-7.00019-3
- language
- English
- LU publication?
- yes
- id
- 0da3c713-dfab-46f6-93c2-75ba887ac8ed
- date added to LUP
- 2025-01-24 14:45:23
- date last changed
- 2025-05-31 00:45:20
@inbook{0da3c713-dfab-46f6-93c2-75ba887ac8ed,
abstract = {{<p>Calcitonin gene-related peptide (CGRP) was suggested to play an important role in primary headaches as far back as 1985 and has been confirmed as playing a significant role in migraine pathophysiology. CGRP receptor antagonists are becoming more and more important for treatment of acute migraine attacks and for prophylaxis of episodic and chronic migraine. The development of drugs that bind CGRP or its canonical receptor are monoclonal antibodies for prophylaxis and small molecular gepants, that block the receptor, acting both in acute attacks of migraine and in prophylaxis. They have all been shown to relieve migraine pain in clinical trials, and their molecular mechanisms involve binding and inhibiting CGRP receptors in the trigeminovascular system. The current view on migraine pathology suggests that binding CGRP receptors on the Aδ-neurons is the main molecular site by which they exhibit their beneficial effects. Here the background to the small molecular gepants is provided and followed by description of the recent phase III data on the second generation of gepants designed for use in acute attacks: ubrogepant, rimegepant and zavegepant. They have all been found effective with minor side-effects and can safely be combined with previously approved medications which provide the patients with novel ways to alleviate their migraine.</p>}},
author = {{Edvinsson, Lars}},
booktitle = {{Migraine Pain Management : Current Pharmacological and Non-pharmacological Options}},
isbn = {{9780443247057}},
keywords = {{CGRP; CGRP receptor; Gepant; Migraine; Pathophysiology; Trigeminovascular system}},
language = {{eng}},
pages = {{295--304}},
publisher = {{Elsevier}},
title = {{Gepants}},
url = {{http://dx.doi.org/10.1016/B978-0-443-24705-7.00019-3}},
doi = {{10.1016/B978-0-443-24705-7.00019-3}},
year = {{2025}},
}