Reactome | CALCR binds gepants

CALCR binds gepants

Stable Identifier

R-HSA-9702849

Type

Reaction [binding]

Species

Homo sapiens

Compartment

extracellular region, plasma membrane

ReviewStatus

5/5

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Migraine is the most common neurological disorder. First- and second-generation calcitonin gene-related peptide (CALCR) receptor antagonists, collectively named gepants, is a class of drugs primarily developed for the acute treatment of migraine. Olcegepant was the first potent and selective non-peptide antagonist of CALCR, formulated the treatment of migraine. In a phase II clinical trial, olcegepant reduced the severity of headache in 60% of migraine sufferers (Recober & Russo 2007). Telcagepant (Chan et al. 2010, Croop et al. 2019), rimegepant (Luo et al. 2012) and ubrogepant (Dodick et al. 2019) are CALCR antagonists that all demonstrate clinical efficacy in the treatment of acute migraine. Atogepant has a longer half-life than other gepants, and is in early phase development for migraine prevention (Chan & Goadsby 2019).

Literature References

PubMed ID	Title	Journal	Year
31800988	Ubrogepant for the Treatment of Migraine Dodick, DW, Lipton, RB, Ailani, J, Lu, K, Finnegan, M, Trugman, JM, Szegedi, A	N. Engl. J. Med.	2019
31311674	Efficacy, safety, and tolerability of rimegepant orally disintegrating tablet for the acute treatment of migraine: a randomised, phase 3, double-blind, placebo-controlled trial Croop, R, Goadsby, PJ, Stock, DA, Conway, CM, Forshaw, M, Stock, EG, Coric, V, Lipton, RB	Lancet	2019
17665333	Olcegepant, a non-peptide CGRP1 antagonist for migraine treatment Recober, A, Russo, AF	IDrugs	2007
20573757	Characterization of the calcitonin gene-related peptide receptor antagonist telcagepant (MK-0974) in human isolated coronary arteries Chan, KY, Edvinsson, L, Eftekhari, S, Kimblad, PO, Kane, SA, Lynch, J, Hargreaves, RJ, de Vries, R, Garrelds, IM, van den Bogaerdt, AJ, Danser, AH, Maassenvandenbrink, A	J. Pharmacol. Exp. Ther.	2010
23153230	Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in clinical trials for treating migraine Luo, G, Chen, L, Conway, CM, Denton, R, Keavy, D, Signor, L, Kostich, W, Lentz, KA, Santone, KS, Schartman, R, Browning, M, Tong, G, Houston, JG, Dubowchik, GM, Macor, JE	J. Med. Chem.	2012
31556018	Recent Advances in Pharmacotherapy for Episodic Migraine Chan, C, Goadsby, PJ	CNS Drugs	2019