G protein-coupled receptors (GPCRs), which mediate the transduction of various extracellular signals to the cell’s interior, belong to one of the largest protein superfamilies in the mammalian genome. As many of these receptors are involved in various physiological processes, they are often targeted in development of therapeutic drugs (Odoemelam et al., 2020). Namely, the calcitonin-gene related peptide receptor has been implicated in migraine pathology and therefore is a target in migraine prophylaxis. Recently, monoclonal antibodies targeting this receptor (anti-CGRP mAbs) have been shown to be effective for this purpose (Bhakta et al., 2021). Nevertheless, more tests examining their efficacy and safety are needed. Firstly, this review article summarises the structure and function of GPCRs, outlining structural characterisation and mode of activation of CGRPRs. Then, it compares the differences in mechanisms of action, efficacy, and safety of different therapeutic drugs for migraine treatment, including anti-CGRP mAbs.