Introduction: Migraine afflicts approximately 11% of the population worldwide producing substantial disability, resulting in loss of productivity both at home and at the workplace. Calcitonin gene-related peptide (CGRP) is closely involved in the cascade of molecular events leading to migraine painful crisis. Areas covered: Acute treatment of migraine is actually based on the use of triptans, class drug which presents a clear limitation due to its cardiovascular side effects. Gepants, a CGRP antagonist class, might offer a new non-vasoconstrictive approach in the acute treatment of migraine. Four chemically unrelated CGRP receptor (CGRP-R) antagonists (olcegepant, telcagepant, MK-3207 and BI 44370 TA) have displayed efficacy in the treatment of migraine. Expert opinion: When compared with triptans, gepants class showed a similar efficacy, moreover corresponding to the best published results for oral triptans. CGRP antagonists are in different phases of their development, and the treatment of migraine could be based on the use of gepants, as class of acute medications. However, CGRP-R antagonists clinical trials seem to be discouraging for their forthcoming use in clinical practice. New CGRP-R antagonists, such as BMS-927711 and BI 44370 TA, are in the pipeline and their developments will outline the future of this drug class.

CGRP receptor antagonists. an expanding drug class for acute migraine? / Negro, Andrea; Luana, Lionetto; Simmaco, Maurizio; Martelletti, Paolo. - In: EXPERT OPINION ON INVESTIGATIONAL DRUGS. - ISSN 1354-3784. - STAMPA. - 21:6(2012), pp. 807-818. [10.1517/13543784.2012.681044]

CGRP receptor antagonists. an expanding drug class for acute migraine?

NEGRO, ANDREA
Primo
Writing – Original Draft Preparation
;
SIMMACO, Maurizio;MARTELLETTI, Paolo
2012

Abstract

Introduction: Migraine afflicts approximately 11% of the population worldwide producing substantial disability, resulting in loss of productivity both at home and at the workplace. Calcitonin gene-related peptide (CGRP) is closely involved in the cascade of molecular events leading to migraine painful crisis. Areas covered: Acute treatment of migraine is actually based on the use of triptans, class drug which presents a clear limitation due to its cardiovascular side effects. Gepants, a CGRP antagonist class, might offer a new non-vasoconstrictive approach in the acute treatment of migraine. Four chemically unrelated CGRP receptor (CGRP-R) antagonists (olcegepant, telcagepant, MK-3207 and BI 44370 TA) have displayed efficacy in the treatment of migraine. Expert opinion: When compared with triptans, gepants class showed a similar efficacy, moreover corresponding to the best published results for oral triptans. CGRP antagonists are in different phases of their development, and the treatment of migraine could be based on the use of gepants, as class of acute medications. However, CGRP-R antagonists clinical trials seem to be discouraging for their forthcoming use in clinical practice. New CGRP-R antagonists, such as BMS-927711 and BI 44370 TA, are in the pipeline and their developments will outline the future of this drug class.
2012
cgrp receptor antagonists; calcitonin gene-related peptide; migraine; cgrp receptor; gepants
01 Pubblicazione su rivista::01g Articolo di rassegna (Review)
CGRP receptor antagonists. an expanding drug class for acute migraine? / Negro, Andrea; Luana, Lionetto; Simmaco, Maurizio; Martelletti, Paolo. - In: EXPERT OPINION ON INVESTIGATIONAL DRUGS. - ISSN 1354-3784. - STAMPA. - 21:6(2012), pp. 807-818. [10.1517/13543784.2012.681044]
File allegati a questo prodotto
File Dimensione Formato  
Negro_CGRP-receptor_2012.pdf

solo gestori archivio

Tipologia: Versione editoriale (versione pubblicata con il layout dell'editore)
Licenza: Tutti i diritti riservati (All rights reserved)
Dimensione 6.63 MB
Formato Adobe PDF
6.63 MB Adobe PDF   Contatta l'autore

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/448440
Citazioni
  • ???jsp.display-item.citation.pmc??? 13
  • Scopus 65
  • ???jsp.display-item.citation.isi??? 59
social impact