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Review

CGRP inhibitors for migraine prophylaxis: a safety review

, & ORCID Icon
Pages 1237-1250 | Received 09 Jun 2020, Accepted 13 Aug 2020, Published online: 21 Sep 2020

Figures & data

Figure 1. An overview of some antimigraine drugs that directly block CGRP or its receptor. Since CGRP plays an important role in the pathophysiology of migraine, in the last decades new antimigraine drugs have been developed for migraine treatment. These drugs include: (i) gepants, which act by directly blocking the CGRP receptor (i.e. rimegepant and atogepant); and (ii) monoclonal antibodies, which directly block CGRP (i.e. eptinezumab, fremanezumab and galcanezumab) or its receptor (i.e. erenumab). CLR, calcitonin receptor-like receptor; RAMP1, receptor activity-modifying protein 1

Figure 1. An overview of some antimigraine drugs that directly block CGRP or its receptor. Since CGRP plays an important role in the pathophysiology of migraine, in the last decades new antimigraine drugs have been developed for migraine treatment. These drugs include: (i) gepants, which act by directly blocking the CGRP receptor (i.e. rimegepant and atogepant); and (ii) monoclonal antibodies, which directly block CGRP (i.e. eptinezumab, fremanezumab and galcanezumab) or its receptor (i.e. erenumab). CLR, calcitonin receptor-like receptor; RAMP1, receptor activity-modifying protein 1

Table 1. The new antimigraine drugs targeting CGRP or its receptor

Figure 2. Composition of the human calcitonin-family receptors and the relative affinity/potency of binding of CGRP, AM and AMY to canonical and non-canonical receptors. CGRP can exert its pathophysiological effects via the activation of its receptor (CGRP receptor) or via the activation of distinct CGRP-responsive receptors with moderate affinity/potency for AM receptors, and practically the same potency for the AMY receptors, as compared to their endogenous ligands. CGRP, calcitonin gene-related peptide; AM, adrenomedullin; AMY, amylin; CLR, calcitonin receptor-like receptor; CTR, calcitonin receptor; RAMP, receptor activity-modifying protein. Human and *rodents values of apKi, bpEC50, and cpKd [Citation98,Citation100]

Figure 2. Composition of the human calcitonin-family receptors and the relative affinity/potency of binding of CGRP, AM and AMY to canonical and non-canonical receptors. CGRP can exert its pathophysiological effects via the activation of its receptor (CGRP receptor) or via the activation of distinct CGRP-responsive receptors with moderate affinity/potency for AM receptors, and practically the same potency for the AMY receptors, as compared to their endogenous ligands. CGRP, calcitonin gene-related peptide; AM, adrenomedullin; AMY, amylin; CLR, calcitonin receptor-like receptor; CTR, calcitonin receptor; RAMP, receptor activity-modifying protein. Human and *rodents values of apKi, bpEC50, and cpKd [Citation98,Citation100]

Table 2. Overview of side effects reported for the prophylactuc anti-migraine drugs