Calcitonin gene-related peptide receptor antagonist

Source: Wikipedia, the free encyclopedia.

Calcitonin gene-related peptide (CGRP) receptor antagonists are a class of drugs that act as

calcitonin gene-related peptide receptor
(CGRPR).

Several

antimigraine agents.[2][3][4] Drugs of this class have also been investigated for use in osteoarthritis.[5]

Examples

Non-peptide small molecules

Monoclonal antibodies targeting the CGRP receptor

  • Erenumab (AMG-334) is approved for prevention of migraine.[14]

Monoclonal antibodies targeting the CGRP molecule

Necrotizing fasciitis

A study has found

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.[19]
Botox blocks the CGRP cascade of nerve cells.

Migraine

As of 2018, erenumab, brand name Aimovig, was approved in the U.S. for use for migraines. It interacts by blocking the CGRP receptor.[20] As of 2018, fremanezumab, brand name Ajovy, was approved in the U.S. for use for migraines. It interacts with the CGRP protein expressed during an attack.[21] The third approved treatment, as of 2018, galcanezumab, brand name Emgality, was approved in the U.S. for use in migraines. It also interacts with the protein.[22]

As of February 2020, eptinezumab (Vyepti) was approved by the FDA for the treatment of migraine via intravenous infusion as well.[23]

Three small-molecule antagonists have been approved for treatment of migraine: ubrogepant, rimegepant, and atogepant.[3][2][4] Ubrogepant and rimegepant are approved for acute treatment.[3][2] Atogepant and rimegepant are approved for preventative treatment.[4][2]

References

  1. U.S. Food and Drug Administration. 2018. Archived
    (PDF) from the original on 2018-12-07.
  2. ^
    U.S. Food and Drug Administration. June 2021. Archived
    (PDF) from the original on 2021-05-28.
  3. ^
    U.S. Food and Drug Administration. 2019. Archived
    (PDF) from the original on 2020-07-17.
  4. ^
    U.S. Food and Drug Administration. March 2022. Archived
    (PDF) from the original on 2021-11-14.
  5. PMID 26686833
    .
  6. PMID 21383046
    .
  7. PMID 23965396
    .
  8. ^ https://www.accessdata.fda.gov/drugsatfda_docs/appletter/2023/216386Orig1s000ltr.pdf
  9. ^ "Pfizer's ZAVZPRET™ (Zavegepant) Migraine Nasal Spray Receives FDA Approval" (Press release). 10 March 2023.
  10. ^ "Press release: Merck Announces Second Quarter 2011 Financial Results". Merck. July 29, 2011. Archived from the original on April 12, 2013.
  11. PMID 17665333
    .
  12. PMID 21172952
    .
  13. PMID 25377933
    .
  14. S2CID 46105364
    .
  15. U.S. Food and Drug Administration. 2020. Archived
    (PDF) from the original on 2020-02-25.
  16. ^ H. Spreitzer (29 February 2016). "Neue Wirkstoffe – TEV-48125". Österreichische Apothekerzeitung (in German) (5/2016): 12.
  17. S2CID 8550606
    .
  18. ^ "Drug Approval Package: Emgality (galcanezumab-gnlm)". www.accessdata.fda.gov. Retrieved 2021-07-09.
  19. ^ "How the germ behind flesh-eating disease hijacks neurons to avoid immune destruction".
  20. ^ Rosenberg, J. (18 May 2018). "FDA Approves Erenumab, First CGRP Inhibitor for Prevention of Migraine". AJMC. Retrieved 6 April 2019.
  21. ^ "FDA Approves Second Anti-CGRP Treatment for Migraine". American Migraine Foundation. Retrieved 6 April 2019.
  22. ^ "Lilly's Emgality (galcanezumab-gnlm) Receives U.S. FDA Approval for the Preventive Treatment of Migraine in Adults". Eli Lilly and Company. Retrieved 6 April 2019.
  23. ^ "Eptinezumab-jjmr (Vyepti) Approved By FDA for Migraine Prevention". American Headache Society. Retrieved 2021-07-09.
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