Calcitonin gene-related peptide receptor antagonist

Calcitonin gene-related peptide receptor antagonist
Drug class
Names
Other namesCGRP-inhibitor

Calcitonin gene-related peptide (CGRP) receptor antagonists are a class of medications that act as blockers of the calcitonin gene-related peptide receptor (CGRPR). They can decrease chronic migraines by one to two episodes per month.[1] They are generally a second line agent after medications such as propranolol and tricyclic antidepressants.[1]

Several monoclonal antibodies that bind to the CGRP receptor or peptide are used to prevention migraines.[2] Three small molecule CGRPR antagonists are approved in the U.S. as antimigraine agents.[3][4][5]

In Canada they cost about 7,000 CAD per year as of 2021.[1]

Medical uses

In 2018, erenumab, galcanezumab, and fremanezumab were approved in the USA for migraines.[6][7][8]

In 2020, eptinezumab was approved by the FDA for the treatment of migraine via intravenous infusion.[9]

Three small-molecule antagonists have been approved for treatment of migraine: ubrogepant, rimegepant, and atogepant.[4][3][5] Ubrogepant and rimegepant are approved for acute treatment.[4][3] Atogepant and rimegepant are approved for preventative treatment.[5][3]

Examples

Non-peptide small molecules

Monoclonal antibodies

Research

Mice given a CGRP receptor antagonist improved insulin secretion and reduced chronic inflammation, improving the metabolic health of the animals.[24] They have also been investigated for use in osteoarthritis.[25]

References

  1. 1 2 3 Ton, Joey (23 August 2021). "#296 Frequent migraines are a headache: Can biologics help?". CFPCLearn. Archived from the original on 28 March 2023. Retrieved 15 June 2023.
  2. "Erenumab (AIMOVIG) Prescribing Information" (PDF). FDA.gov. U.S. Food and Drug Administration. 2018. Archived (PDF) from the original on 2018-12-07.
  3. 1 2 3 4 5 "Nurtec ODT Prescribing Information" (PDF). FDA.gov. U.S. Food and Drug Administration. June 2021. Archived (PDF) from the original on 2021-05-28.
  4. 1 2 3 4 "Ubrogepant Prescribing Information" (PDF). FDA.gov. U.S. Food and Drug Administration. 2019. Archived (PDF) from the original on 2020-07-17.
  5. 1 2 3 4 "Qulipta Prescribing Information" (PDF). FDA.gov. U.S. Food and Drug Administration. March 2022. Archived (PDF) from the original on 2021-11-14.
  6. Rosenberg, J. "FDA Approves Erenumab, First CGRP Inhibitor for Prevention of Migraine". AJMC. Archived from the original on 24 February 2019. Retrieved 6 April 2019.
  7. "FDA Approves Second Anti-CGRP Treatment for Migraine". American Migraine Foundation. Archived from the original on 24 February 2019. Retrieved 6 April 2019.
  8. "Lilly's Emgality (galcanezumab-gnlm) Receives U.S. FDA Approval for the Preventive Treatment of Migraine in Adults". Eli Lilly and Company. Archived from the original on 24 February 2019. Retrieved 6 April 2019.
  9. "Eptinezumab-jjmr (Vyepti) Approved By FDA for Migraine Prevention". American Headache Society. Archived from the original on 2021-10-19. Retrieved 2021-07-09.
  10. 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.
  11. 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.
  12. "Press release: Merck Announces Second Quarter 2011 Financial Results". Merck. July 29, 2011. Archived from the original on April 12, 2013.
  13. 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.
  14. 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.
  15. 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.
  16. "Archive copy". Archived from the original on 2023-04-08. Retrieved 2023-05-22.{{cite web}}: CS1 maint: archived copy as title (link)
  17. "Archive copy" (PDF). Archived (PDF) from the original on 2023-03-11. Retrieved 2023-05-22.{{cite web}}: CS1 maint: archived copy as title (link)
  18. "Archive copy". Archived from the original on 2023-04-08. Retrieved 2023-05-22.{{cite web}}: CS1 maint: archived copy as title (link)
  19. Mitsikostas, DD; Reuter, U (2017). "Calcitonin gene-related peptide monoclonal antibodies for migraine prevention: comparisons across randomized controlled studies". Curr Opin Neurol. 30 (3): 272–280. doi:10.1097/WCO.0000000000000438. PMID 28240610.
  20. "Eptinezumab Prescribing Information" (PDF). FDA.gov. U.S. Food and Drug Administration. 2020. Archived (PDF) from the original on 2020-02-25.
  21. H. Spreitzer (29 February 2016). "Neue Wirkstoffe – TEV-48125". Österreichische Apothekerzeitung (in German) (5/2016): 12.{{cite journal}}: CS1 maint: unrecognized language (link)
  22. 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.
  23. "Drug Approval Package: Emgality (galcanezumab-gnlm)". www.accessdata.fda.gov. Archived from the original on 2019-12-07. Retrieved 2021-07-09.
  24. Riera CE, Huising MO, Follett P, Leblanc M, Halloran J, Van Andel R, de Magalhaes Filho CD, Merkwirth C, Dillin A (2014). "TRPV1 pain receptors regulate longevity and metabolism by neuropeptide signaling". Cell. 157 (5): 1023–1036. doi:10.1016/j.cell.2014.03.051. PMID 24855942.
  25. 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 (7): 1177–84. doi:10.1002/jor.23132. PMID 26686833.


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