Calcitonin gene-related peptide (CGRP) is a 37-amino acid neuropeptide. It has two forms: α and β. CGRP is widely expressed in the central and peripheral nervous systems. Great attention is paid to examining the role of CGRP in pain transmission, including modulation of the function of other neurotransmitters. CGRP is regarded as a key mediator in pain response; it is released from the trigeminovascular system after stimulation of sensory nerve endings. It is well documented that CGRP has a very important role in the pathogenesis of migraine. The concentration of CGRP increases in response to stimulation of the trigeminal ganglion. CGRP may affect the activity of sensory neurons by direct control of the pain response in the course of a migraine attack. Therefore, trials are being conducted to develop effective medicines, which could block CGRP’s activity or decrease its concentration. The efficacy of a few CGRP receptor antagonists in the treatment of migraine has been demonstrated in clinical trials. The potential use of monoclonal antibodies directed against CGRP or its receptors is also highlighted. They should decrease severity and frequency of migraine attacks by reducing the levels of CGRP or block its action. These drugs can become an effective alternative to triptans in migraine treatment and to other medicines used in the treatment of disorders associated with dysfunction of the trigeminal nerve.