Calcitonin gene-related peptide receptor antagonist
Calcitonin gene-related peptide (CGRP) receptor antagonists are a class of drugs that act as antagonists of the calcitonin gene-related peptide receptor (CGRPR).
CGRPR antagonists are under investigation as potential antimigraine agents and also in the context of osteoarthritis.[1]
Examples
- olcegepant (BIBN-4096BS),
- telcagepant (MK-0974), reached phase III clinical trials - now abandoned,
- ubrogepant,[2]
- LY2951742 (by Eli Lilly & Co)
TEV-48125 is not a Calcitonin gene-related peptide receptor antagonist but a monoclonal antibody targeting CGRP .[3][4] Most experimental CGRP inhibitors are monoclonal antibodies[5] given by monthly injections.[5]
Clinical trials
In June 2015 Phase 2 clinical trial data for three different anti-CGRP drugs ( Amgen (AMG 334), Teva Pharmaceuticals (TEV-48125), and Eli Lilly & Co (LY2951742)) were presented at the American Headache Society's (AHS) annual meeting.[5]
In March 2016 Alder reported phase IIb clinical trial data for its ALD403.[6]
By April 2016, Alder, Amgen and Teva had initiated phase III trials.[7]
References
- ↑ Nakasa, T; Ishikawa, M; Takada, T; Miyaki, S; Ochi, M (2015). "Attenuation of cartilage degeneration by calcitonin gene-related paptide receptor antagonist via inhibition of subchondral bone sclerosis in osteoarthritis mice". Journal of Orthopaedic Research: n/a. doi:10.1002/jor.23132. PMID 26686833.
- ↑ Tfelt-Hansen, P; Olesen, J (Apr 2011). "Possible site of action of CGRP antagonists in migraine.". Cephalalgia: an international journal of headache. 31 (6): 748–50. doi:10.1177/0333102411398403. PMID 21383046.
- ↑ H. Spreitzer (29 February 2016). "Neue Wirkstoffe – TEV-48125". Österreichische Apothekerzeitung (in German) (5/2016): 12.
- ↑ Walter, S; Bigal, M. E. (2015). "TEV-48125: a review of a monoclonal CGRP antibody in development for the preventive treatment of migraine". Current Pain and Headache Reports. 19 (3): 6. doi:10.1007/s11916-015-0476-1. PMID 25754596.
- 1 2 3 New Data on CGRP Monoclonal Antibodies for Migraine Prevention. June 2015
- ↑ Alder Reports Phase 2b Trial of ALD403 Meets Primary and Secondary Endpoints Demonstrating Migraine Prevention in Patients with Chronic Migraine. March 2016
- ↑ Can Alder Beat Teva And Amgen In Treating Migraines? Will Positive Phase III Data Help Keryx's Auryxia Receive Approval For An Expanded Indication? April 2016