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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