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词条 Calcitonin gene-related peptide receptor antagonist
释义

  1. Examples

      Non-peptide small molecules   Monoclonal antibodies targeting the CGRP receptor  Monoclonal antibodies targeting the CGRP molecule  Necrotizing Fasciitis 

  2. Migraine

  3. References

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

  • BI 44370 TA (BI 44370)[2]
  • MK-3207[3]
  • Olcegepant (BIBN-4096BS)[4]
  • Rimegepant (BMS-927711)[5]
  • SB-268262
  • Telcagepant (MK-0974), reached phase III clinical trials and was discontinued in 2011.[6]
  • Ubrogepant[7]

Monoclonal antibodies targeting the CGRP receptor

  • Erenumab (AMG-334)[8]

Monoclonal antibodies targeting the CGRP molecule

  • Eptinezumab (ALD403)
  • Fremanezumab (TEV-48125)[9][10]
  • Galcanezumab (LY2951742)

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.

Migraine

As of 2018, Erenumaub, trade name Aimovig, was approved in the U.S. for use for migraines. It interacts by blocking the CGRP receptor.[12] As of 2018, Fremanezumab, trade name Ajovy, was approve in the U.S. for use for migraines. It interacts with the CGRP protein with is expressed during an attack.[13] The third approved treatment, as of 2018, Galcanezumab, trade name Emgality, was approved in the U.S. for use in migraines. It also interacts with the protein.[14]

References

1. ^{{Cite journal|pmid=26686833|year=2015|author1=Nakasa|first1=T|title=Attenuation of cartilage degeneration by calcitonin gene-related paptide receptor antagonist via inhibition of subchondral bone sclerosis in osteoarthritis mice|journal=Journal of Orthopaedic Research|pages=1177–84|last2=Ishikawa|first2=M|last3=Takada|first3=T|last4=Miyaki|first4=S|last5=Ochi|first5=M|doi=10.1002/jor.23132|volume=34|issue=7}}
2. ^{{cite journal | last1 = Diener | first1 = HC | last2 = Barbanti | first2 = P | last3 = Dahlöf | first3 = C | last4 = Reuter | first4 = U | last5 = Habeck | first5 = J | last6 = Podhorna | first6 = J | title = BI 44370 TA, an Oral CGRP Antagonist for the Treatment of Acute Migraine Attacks: Results From a Phase II Study | journal = Cephalalgia: An International Journal of Headache | date = April 2011 | volume = 31 | issue = 5 | pages = 573–84 | doi = 10.1177/0333102410388435 | pmid = 21172952 }}
3. ^{{cite journal | last1 = Li | first1 = CC | last2 = Vermeersch | first2 = S | last3 = Denney | first3 = WS | last4 = Kennedy | first4 = WP | last5 = Palcza | first5 = J | last6 = Gipson | first6 = A | last7 = Han | first7 = TH | last8 = Blanchard | first8 = R | last9 = De Lepeleire | first9 = I | last10 = Depré | first10 = M | last11 = Murphy | first11 = MG | last12 = Van Dyck | first12 = K | last13 = de Hoon | first13 = JN | title = Characterizing the PK/PD Relationship for Inhibition of Capsaicin-Induced Dermal Vasodilatation by MK-3207, an Oral Calcitonin Gene Related Peptide Receptor Antagonist | journal = British Journal of Clinical Pharmacology | date = May 2015 | volume = 79 | issue = 5 | pages = 831–7 | doi = 10.1111/bcp.12547 | pmid = 25377933 | pmc = 4415719}}
4. ^{{cite journal | last1 = Recober | first1 = A | last2 = Russo | first2 = AF | title = Olcegepant, a Non-Peptide CGRP1 Antagonist for Migraine Treatment | journal = IDrugs: The Investigational Drugs Journal | date = August 2007 | volume = 10 | issue = 8 | pages = 566–74 | pmid = 17665333 }}
5. ^{{cite journal | last1 = Marcus | first1 = R | last2 = Goadsby | first2 = PJ | last3 = Dodick | first3 = D | last4 = Stock | first4 = D | last5 = Manos | first5 = G | last6 = Fischer | first6 = TZ | title = BMS-927711 for the Acute Treatment of Migraine: a Double-Blind, Randomized, Placebo Controlled, Dose-Ranging Trial | journal = Cephalalgia: An International Journal of Headache | date = February 2014 | volume = 34 | issue = 2 | pages = 114–25 | doi = 10.1177/0333102413500727 | pmid = 23965396 }}
6. ^{{cite news|title=Press release: Merck Announces Second Quarter 2011 Financial Results|url=http://www.mercknewsroom.com/press-release/financial-news/merck-announces-second-quarter-2011-financial-results|work=Merck|date=July 29, 2011|archiveurl=https://web.archive.org/web/20130412063354/http://www.mercknewsroom.com/press-release/financial-news/merck-announces-second-quarter-2011-financial-results|archivedate=April 12, 2013}}
7. ^{{cite journal | last1 = Tfelt-Hansen | first1 = P | last2 = Olesen | first2 = J | title = Possible Site of Action of CGRP Antagonists in Migraine | journal = Cephalalgia: An International Journal of Headache | date = April 2011 | volume = 31 | issue = 6 | pages = 748–50 | doi = 10.1177/0333102411398403 | pmid = 21383046}}
8. ^{{cite journal | pmid = 28240610 | doi=10.1097/WCO.0000000000000438 | volume=30 | issue=3 | title=Calcitonin gene-related peptide monoclonal antibodies for migraine prevention: comparisons across randomized controlled studies | journal=Curr Opin Neurol | pages=272–280 | last1 = Mitsikostas | first1 = DD | last2 = Reuter | first2 = U| year=2017 }}
9. ^{{cite journal| author = H. Spreitzer| date = 29 February 2016| title = Neue Wirkstoffe – TEV-48125| journal = Österreichische Apothekerzeitung| issue = 5/2016| page = 12| language = German}}
10. ^{{cite journal | last1 = Walter | first1 = S | last2 = Bigal | first2 = ME | title = TEV-48125: a Review of a Monoclonal CGRP Antibody in Development for the Preventive Treatment of Migraine | journal = Current Pain and Headache Reports | date = March 2015 | volume = 19 | issue = 3 | pages = 6 | doi = 10.1007/s11916-015-0476-1 | pmid = 25754596 }}
11. ^{{cite web | url=https://medicalxpress.com/news/2018-05-germ-flesh-eating-disease-hijacks-neurons.html | title=How the germ behind flesh-eating disease hijacks neurons to avoid immune destruction}}
12. ^{{cite web |last1=Rosenberg |first1=J. |title=FDA Approves Erenumab, First CGRP Inhibitor for Prevention of Migraine |url=https://www.ajmc.com/newsroom/fda-approves-erenumab-first-cgrp-inhibitor-for-prevention-of-migraine |website=AJMC |accessdate=6 April 2019}}
13. ^{{cite web |title=FDA Approves Second Anti-CGRP Treatment for Migraine |url=https://americanmigrainefoundation.org/resource-library/fda-approves-second-anti-cgrp-treatment-for-migraine/ |website=American Migraine Foundation |accessdate=6 April 2019}}
14. ^{{cite web |title=Lilly's Emgality™ (galcanezumab-gnlm) Receives U.S. FDA Approval for the Preventive Treatment of Migraine in Adults |url=https://investor.lilly.com/news-releases/news-release-details/lillys-emgalitytm-galcanezumab-gnlm-receives-us-fda-approval |website=Eli Lilly and Company |accessdate=6 April 2019}}
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3 : Antimigraine drugs|Receptor antagonists|Calcitonin gene-related peptide receptor antagonists
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