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Calcitonin gene-related peptide receptor antagonist

January 01, 1970

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

Several monoclonal antibodies that bind to the CGRP receptor or peptide have been approved for prevention of migraine.[1] Three small molecule CGRPR antagonists are approved in the U.S. as antimigraine agents.[2][3][4] Drugs of this class have also been investigated for use in osteoarthritis.[5]

Examples edit

Non-peptide small molecules edit

  • Ubrogepant is approved for acute treatment of migraines[6][3]
  • Rimegepant (BMS-927711) is approved for acute and preventative treatment of migraines[7][2]
  • Atogepant (AGN-241689) is approved for preventative treatment of migraines[4]
  • Zavegepant (BHV- 3500) is a nasal spray approved for acute treatment of migraines.[8][9]
  • Telcagepant (MK-0974), reached phase III clinical trials; development discontinued in 2011.[10]
  • Olcegepant (BIBN-4096BS) is a drug candidate[11]
  • BI 44370 TA (BI 44370)[12]
  • MK-3207[13]
  • SB-268262

Monoclonal antibodies targeting the CGRP receptor edit

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

Monoclonal antibodies targeting the CGRP molecule edit

Necrotizing fasciitis edit

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

Migraine edit

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 edit

  1. ^ "Erenumab (AIMOVIG) Prescribing Information" (PDF). FDA.gov. U.S. Food and Drug Administration. 2018. (PDF) from the original on 2018-12-07.
  2. ^ a b c d e "Nurtec ODT Prescribing Information" (PDF). FDA.gov. U.S. Food and Drug Administration. June 2021. (PDF) from the original on 2021-05-28.
  3. ^ a b c d "Ubrogepant Prescribing Information" (PDF). FDA.gov. U.S. Food and Drug Administration. 2019. (PDF) from the original on 2020-07-17.
  4. ^ a b c d "Qulipta Prescribing Information" (PDF). FDA.gov. U.S. Food and Drug Administration. March 2022. (PDF) from the original on 2021-11-14.
  5. ^ 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.
  6. ^ 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.
  7. ^ 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.
  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. ^ . Merck. July 29, 2011. Archived from the original on April 12, 2013.
  11. ^ 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.
  12. ^ 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.
  13. ^ 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.
  14. ^ 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. S2CID 46105364.
  15. ^ "Eptinezumab Prescribing Information" (PDF). FDA.gov. U.S. Food and Drug Administration. 2020. (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. ^ 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. 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.

January 01, 1970
calcitonin, gene, related, peptide, receptor, antagonist, calcitonin, gene, related, peptide, cgrp, receptor, antagonists, class, drugs, that, antagonists, calcitonin, gene, related, peptide, receptor, cgrpr, several, monoclonal, antibodies, that, bind, cgrp, . Calcitonin gene related peptide CGRP receptor antagonists are a class of drugs that act as antagonists of the calcitonin gene related peptide receptor CGRPR Several monoclonal antibodies that bind to the CGRP receptor or peptide have been approved for prevention of migraine 1 Three small molecule CGRPR antagonists are approved in the U S as antimigraine agents 2 3 4 Drugs of this class have also been investigated for use in osteoarthritis 5 Contents 1 Examples 1 1 Non peptide small molecules 1 2 Monoclonal antibodies targeting the CGRP receptor 1 3 Monoclonal antibodies targeting the CGRP molecule 1 4 Necrotizing fasciitis 2 Migraine 3 ReferencesExamples editNon peptide small molecules edit Ubrogepant is approved for acute treatment of migraines 6 3 Rimegepant BMS 927711 is approved for acute and preventative treatment of migraines 7 2 Atogepant AGN 241689 is approved for preventative treatment of migraines 4 Zavegepant BHV 3500 is a nasal spray approved for acute treatment of migraines 8 9 Telcagepant MK 0974 reached phase III clinical trials development discontinued in 2011 10 Olcegepant BIBN 4096BS is a drug candidate 11 BI 44370 TA BI 44370 12 MK 3207 13 SB 268262 Monoclonal antibodies targeting the CGRP receptor edit Erenumab AMG 334 is approved for prevention of migraine 14 Monoclonal antibodies targeting the CGRP molecule edit Eptinezumab ALD403 is approved for prevention of migraine 15 Fremanezumab TEV 48125 is approved for prevention of migraine 16 17 Galcanezumab LY2951742 is approved for prevention of migraine and cluster headaches 18 Necrotizing fasciitis edit 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 19 Botox blocks the CGRP cascade of nerve cells Migraine editAs 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 edit Erenumab AIMOVIG Prescribing Information PDF FDA gov U S Food and Drug Administration 2018 Archived PDF from the original on 2018 12 07 a b c d e Nurtec ODT Prescribing Information PDF FDA gov U S Food and Drug Administration June 2021 Archived PDF from the original on 2021 05 28 a b c d Ubrogepant Prescribing Information PDF FDA gov U S Food and Drug Administration 2019 Archived PDF from the original on 2020 07 17 a b c d Qulipta Prescribing Information PDF FDA gov U S Food and Drug Administration March 2022 Archived PDF from the original on 2021 11 14 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 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 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 https www accessdata fda gov drugsatfda docs appletter 2023 216386Orig1s000ltr pdf Pfizer s ZAVZPRET Zavegepant Migraine Nasal Spray Receives FDA Approval Press release 10 March 2023 Press release Merck Announces Second Quarter 2011 Financial Results Merck July 29 2011 Archived from the original on April 12 2013 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 Diener HC Barbanti P Dahlof 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 Li CC Vermeersch S Denney WS Kennedy WP Palcza J Gipson A Han TH Blanchard R De Lepeleire I Depre 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 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 S2CID 46105364 Eptinezumab Prescribing Information PDF FDA gov U S Food and Drug Administration 2020 Archived PDF from the original on 2020 02 25 H Spreitzer 29 February 2016 Neue Wirkstoffe TEV 48125 Osterreichische Apothekerzeitung in German 5 2016 12 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 S2CID 8550606 Drug Approval Package Emgality galcanezumab gnlm www accessdata fda gov Retrieved 2021 07 09 How the germ behind flesh eating disease hijacks neurons to avoid immune destruction Rosenberg J 18 May 2018 FDA Approves Erenumab First CGRP Inhibitor for Prevention of Migraine AJMC Retrieved 6 April 2019 FDA Approves Second Anti CGRP Treatment for Migraine American Migraine Foundation Retrieved 6 April 2019 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 Eptinezumab jjmr Vyepti Approved By FDA for Migraine Prevention American Headache Society Retrieved 2021 07 09 Retrieved from https en wikipedia org w index php title Calcitonin gene related peptide receptor antagonist amp oldid 1214944862, wikipedia, wiki, book, books, library,

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