The locus of action of CGRPergic monoclonal antibodies against migraine: peripheral over central mechanisms.

The locus of action of CGRPergic monoclonal antibodies against migraine: peripheral over central mechanisms. CNS Neurol Disord Drug Targets. 2020 Jun 18;: Authors: González-Hernández A, Marichal-Cancino BA, García-Boll E, Villalón CM Abstract Migraine is a complex neurovascular disorder characterized by attacks of moderate to severe unilateral headache, accompanied by photophobia or other neurological signs. Although an arsenal of antimigraine agents is currently available in the market, not all patients respond to them. As calcitonin gene-related peptide (CGRP) plays a key role in the pathophysiology of migraine, CGRP receptor antagonists (gepants) have been developed. Unfortunately, further pharmaceutical development (for olcegepant and telcagepant) was interrupted due to pharmacokinetic issues observed during the randomized clinical trials (RCT). On this basis, the use of monoclonal antibodies (mAbs; immunoglobulins) against CGRP or its receptor has recently emerged as a novel pharmacotherapy to treat migraine. RCT showed that these mAbs are effective against migraine producing fewer adverse events. Presently, the U.S. Food and Drug Administration approved four mAbs, namely: (i) erenumab; (ii) fremanezumab; (iii) galcanezumab; and (iv) eptinezumab. In general, specific antimigraine compounds exert their action in the trigeminovascular system, but the locus of action (peripheral vs. central) of the mAbs remains elusive. Since t...
Source: CNS and Neurological Disorders Drug Targets - Category: Drugs & Pharmacology Authors: Tags: CNS Neurol Disord Drug Targets Source Type: research