BACKGROUND: Migraine is a debilitating headache disorder which affects 
approximately 12% of the general population and is the cause of significant loss 
of productivity (i.e., lost time from work or school) for those afflicted. The 
current standard of care, the 5-HT(1B/1D) agonists known as triptans, is 
contraindicated in patients with cardiovascular disease due to their inherent 
vasoconstrictive activity; thus, there is a need to develop an alternative 
therapy for the treatment of the disorder.
OBJECTIVE: This article reviews patent publications related to the use of small 
molecule calcitonin gene-related peptide (CGRP) receptor antagonists for the 
treatment of migraine that have appeared in the literature within the past 
decade. The commentary is supplemented by information presented in journal 
articles and focuses on the activity of several major pharmaceutical companies 
in the field.
CONCLUSION: Two small molecule CGRP receptor antagonists, olcegepant and 
telcagepant, have been shown to be clinically efficacious in the treatment of 
migraine, and thus provide validation of this novel therapeutic mechanism.