Calcitonin gene-related peptide receptor antagonist

Calcitonin gene-related peptide (CGRP) receptor antagonists are a class of drug candidates 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

Necrotizing Fasciitis

A study has found botox effective against necrotizing fasciitis caused by S. pyogenes in mice. Its mechanism of action is by blocking CGRP receptor of nerve cells, which trigger intense pain and activate CGRP cascade, which prevents the immune system attacks to control the pathogen.[11] Botox blocks the CGRP cascade of nerve cells.

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. doi:10.1002/jor.23132. PMID 26686833.
  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. doi:10.1177/0333102410388435. PMID 21172952.
  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. doi:10.1111/bcp.12547. PMC 4415719. PMID 25377933.
  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. doi:10.1177/0333102413500727. PMID 23965396.
  6. ↑ "Press release: Merck Announces Second Quarter 2011 Financial Results". Merck. July 29, 2011. Archived from the original on April 12, 2013.
  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. doi:10.1177/0333102411398403. PMID 21383046.
  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. doi:10.1097/WCO.0000000000000438. PMID 28240610.
  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. doi:10.1007/s11916-015-0476-1. PMID 25754596.
  11. ↑ https://medicalxpress.com/news/2018-05-germ-flesh-eating-disease-hijacks-neurons.html


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