CGRP Monoclonal Antibodies for Migraine: Rationale and Progress.

07:00 EST 7th November 2017 | BioPortfolio

Summary of "CGRP Monoclonal Antibodies for Migraine: Rationale and Progress."

Calcitonin gene-related peptide (CGRP), a neuropeptide abundant in the trigeminal system and widely expressed in both the peripheral and central nervous systems, has recently emerged as a promising target for migraine management. While known as a potent arterial vasodilator, the role of CGRP in migraine is likely mediated by modulating nociception and sustaining neurogenic inflammation that leads to further peripheral and central pain sensitization. Functional blockade of CGRP, which involves either CGRP receptor antagonists or monoclonal antibodies (mAbs) to CGRP or its receptor, has recently shown clinical efficacy in migraine management. The site of action, although still being studied, is likely in nervous system structures outside the blood-brain barrier. To date, four CGRP function-blocking mAbs (three target CGRP and one targets the CGRP receptor) are under clinical investigation for migraine prophylaxis. Phase II and III studies were promising with favorable safety profiles. CGRP function-blocking mAbs may potentially revolutionize the management of migraine. This review discusses in depth the fundamental role of CGRP in migraine pathogenesis as well as the clinical efficacy of CGRP function-blocking mAbs.


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This article was published in the following journal.

Name: BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy
ISSN: 1179-190X


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Medical and Biotech [MESH] Definitions

Antibodies obtained from a single clone of cells grown in mice or rats.

Antibodies produced by clones of cells such as those isolated after hybridization of activated B LYMPHOCYTES with neoplastic cells. These hybrids are often referred to as HYBRIDOMAS.

Antibodies from non-human species whose protein sequences have been modified to make them nearly identical with human antibodies. If the constant region and part of the variable region are replaced, they are called humanized. If only the constant region is modified they are called chimeric. INN names for humanized antibodies end in -zumab.

Antibodies, often monoclonal, in which the two antigen-binding sites are specific for separate ANTIGENIC DETERMINANTS. They are artificial antibodies produced by chemical crosslinking, fusion of HYBRIDOMA cells, or by molecular genetic techniques. They function as the main mediators of targeted cellular cytotoxicity and have been shown to be efficient in the targeting of drugs, toxins, radiolabeled haptens, and effector cells to diseased tissue, primarily tumors.

Cell surface proteins that bind calcitonin gene-related peptide (CGRP) with high affinity and trigger intracellular changes which influence the behavior of cells. CGRP receptors are present in both the central nervous system and the periphery and are not the same as calcitonin receptors.

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