CGRP receptor antagonists: a new choice for acute treatment of migraine?

The neuropeptide calcitonin gene-related peptide (CGRP) is believed to play a central role in the underlying pathology of migraine. Serum levels of CGRP, elevated during a migraine attack, return to normal as pain alleviates. Recently, a causative role for CGRP in migraine has been suggested. Based on these findings, it was proposed that blockade of postsynaptic CGRP receptors, and hence the physiological effects of CGRP, should effectively abort a migraine attack. This review will discuss the therapeutic potential of olcegepant, the first non-peptide CGRP receptor antagonist available for human studies, within the context of current neurovascular theories on migraine pathology.