title: CGRP receptor antagonists: an expanding drug class for acute migraine?
abstract: BACKGROUND
  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.
  
  
  METHODS
  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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Sapienza University of Rome and Regional Referral Headache Centre, Sant'Andrea Hospital, Department of Clinical and Molecular Medicine, Via di Grottarossa 1035-1039, 00189, Rome, Italy.
authors.forename: Andrea
authors.initials: A
authors.lastname: Negro
authors.forename: Luana
authors.initials: L
authors.lastname: Lionetto
authors.forename: Maurizio
authors.initials: M
authors.lastname: Simmaco
authors.forename: Paolo
authors.initials: P
authors.lastname: Martelletti
mesh_terms: D000818:Animals; D001381:Azepines / Q000494:pharmacology / Q000627:therapeutic use; D000077221:Calcitonin Gene-Related Peptide Receptor Antagonists; D004151:Dipeptides / Q000494:pharmacology / Q000627:therapeutic use; D015195:Drug Design; D006801:Humans; D007093:Imidazoles / Q000494:pharmacology / Q000627:therapeutic use; D008881:Migraine Disorders / Q000188:drug therapy* / Q000503:physiopathology; D010879:Piperazines; D011799:Quinazolines / Q000494:pharmacology / Q000627:therapeutic use; D014363:Tryptamines / Q000009:adverse effects / Q000627:therapeutic use
chemical_list: D001381:Azepines; D000077221:Calcitonin Gene-Related Peptide Receptor Antagonists; D004151:Dipeptides; D007093:Imidazoles; D010879:Piperazines; D011799:Quinazolines; D014363:Tryptamines; C525458:telcagepant; C406305:olcegepant