CALCR binds gepants

Stable Identifier
Reaction [binding]
Homo sapiens
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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

Trugman, JM, Finnegan, M, Lu, K, Lipton, RB, Ailani, J, Dodick, DW, 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

Stock, DA, Goadsby, PJ, Forshaw, M, Lipton, RB, Conway, CM, Croop, R, Stock, EG, Coric, V

Lancet 2019
17665333 Olcegepant, a non-peptide CGRP1 antagonist for migraine treatment

Russo, AF, Recober, A

IDrugs 2007
20573757 Characterization of the calcitonin gene-related peptide receptor antagonist telcagepant (MK-0974) in human isolated coronary arteries

Hargreaves, RJ, Eftekhari, S, Kane, SA, Kimblad, PO, Danser, AH, Chan, KY, Edvinsson, L, Garrelds, IM, Lynch, J, de Vries, R, Maassenvandenbrink, A, van den Bogaerdt, AJ

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

Signor, L, Browning, M, Santone, KS, Conway, CM, Kostich, W, Lentz, KA, Chen, L, Tong, G, Dubowchik, GM, Luo, G, Denton, R, Houston, JG, Keavy, D, Schartman, R, Macor, JE

J. Med. Chem. 2012
31556018 Recent Advances in Pharmacotherapy for Episodic Migraine

Goadsby, PJ, Chan, C

CNS Drugs 2019
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