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

Abstract

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.

Migraine and neuropeptides

“…olcegepant (BIBN4096BS), telcagepant (MK-0974), MK-3207, MK-1602, BMS-694153, BMS-927711 and BI44370TA (Negro et al, 2012). Telcagepant has also been evaluated for the prevention of migraine (Ho et al, 2014).…”

Localization of CGRP, CGRP receptor, PACAP and glutamate in trigeminal ganglion. Relation to the blood–brain barrier

“…Several CGRP receptor antagonists (olcegepant, telcagepant, MK-3207, BI 44370TA and BMS927711) have displayed efficacy in the treatment of migraine Negro et al, 2012;Dolgin, 2013). The CGRP receptor antagonists have potentially opened up a new option in migraine treatment; however, there remains active discussion as to where these molecules act to reduce migraine pain.…”

Anti-CGRP monoclonal antibodies in migraine: current perspectives

“…The recently developed monoclonal antibodies against CGRP or its receptor (anti-CGRP mAbs) have triggered much interest in the headache community. A number of clinical trials have been carried out, are underway, or have been planned in migraine prevention [17][18][19][20][21][22][23]. After a necessary premise on migraine characteristics and current treatment options, as well as notes on pathophysiological mechanisms, particularly in relation to CGRP, the present review will thus focus on the results of the studies on anti-CGRP mAbs, critically discussing the future implications for their systematic employment in migraine management.…”