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

Non-peptide small molecules

Monoclonal antibodies targeting the CGRP receptor

Monoclonal antibodies targeting the CGRP molecule

Most experimental CGRP inhibitors are monoclonal antibodies given by monthly injections.[11]

Clinical trials

In June 2015 Phase II clinical trial data for three different anti-CGRP drugs (Amgen (erenumab), Teva (fremanezumab), and Eli Lilly (galcanezumab)) were presented at the American Headache Society's (AHS) annual meeting.[11]

In March 2016 Alder reported phase IIb clinical trial data for its eptinezumab.[12]

By April 2016, Alder, Amgen and Teva had initiated phase III trials.[13]

References

  1. ↑ 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. 34: 1177–84. PMID 26686833. doi:10.1002/jor.23132.
  2. ↑ Diener, HC; Barbanti, P; Dahlöf, C; Reuter, U; Habeck, J; Podhorna, J (April 2011). "BI 44370 TA, an Oral CGRP Antagonist for the Treatment of Acute Migraine Attacks: Results From a Phase II Study". Cephalalgia: an International Journal of Headache. 31 (5): 573–84. PMID 21172952. doi:10.1177/0333102410388435.
  3. ↑ Li, CC; Vermeersch, S; Denney, WS; Kennedy, WP; Palcza, J; Gipson, A; Han, TH; Blanchard, R; De Lepeleire, I; Depré, M; Murphy, MG; Van Dyck, K; de Hoon, JN (May 2015). "Characterizing the PK/PD Relationship for Inhibition of Capsaicin-Induced Dermal Vasodilatation by MK-3207, an Oral Calcitonin Gene Related Peptide Receptor Antagonist". British Journal of Clinical Pharmacology. 79 (5): 831–7. PMC 4415719 Freely accessible. PMID 25377933. doi:10.1111/bcp.12547.
  4. ↑ Recober, A; Russo, AF (August 2007). "Olcegepant, a Non-Peptide CGRP1 Antagonist for Migraine Treatment". IDrugs: the Investigational Drugs Journal. 10 (8): 566–74. PMID 17665333.
  5. ↑ Marcus, R; Goadsby, PJ; Dodick, D; Stock, D; Manos, G; Fischer, TZ (February 2014). "BMS-927711 for the Acute Treatment of Migraine: a Double-Blind, Randomized, Placebo Controlled, Dose-Ranging Trial". Cephalalgia: an International Journal of Headache. 34 (2): 114–25. PMID 23965396. doi:10.1177/0333102413500727.
  6. ↑ Merck Announces Second Quarter 2011 Financial Results
  7. ↑ Tfelt-Hansen, P; Olesen, J (April 2011). "Possible Site of Action of CGRP Antagonists in Migraine". Cephalalgia: An International Journal of Headache. 31 (6): 748–50. PMID 21383046. doi:10.1177/0333102411398403.
  8. ↑ Mitsikostas, DD; Reuter, U. "Calcitonin gene-related peptide monoclonal antibodies for migraine prevention: comparisons across randomized controlled studies". Curr Opin Neurol. 30: 272–280. PMID 28240610. doi:10.1097/WCO.0000000000000438.
  9. ↑ H. Spreitzer (29 February 2016). "Neue Wirkstoffe – TEV-48125". Österreichische Apothekerzeitung (in German) (5/2016): 12.
  10. ↑ Walter, S; Bigal, ME (March 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. PMID 25754596. doi:10.1007/s11916-015-0476-1.
  11. 1 2 New Data on CGRP Monoclonal Antibodies for Migraine Prevention. June 2015
  12. ↑ Alder Reports Phase 2b Trial of ALD403 Meets Primary and Secondary Endpoints Demonstrating Migraine Prevention in Patients with Chronic Migraine. March 2016
  13. ↑ 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


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