Target intelligence / Profile preview

Beta-calcitonin gene-related peptide (β-CGRP) (β-CGRP)

Target
β-CGRP
Molecular classification
Neuropeptide, Peptide hormone, Calcitonin family
01

Overview

Beta-calcitonin gene-related peptide (β-CGRP) is a 37-amino acid neuropeptide and a member of the calcitonin family, encoded by the CALCB gene (UniProt P06881). It is a potent endogenous vasodilator and plays a critical role in the transmission of nociceptive signals within the trigeminovascular system (Goadsby et al., NEJM 2017). While closely related to α-CGRP, β-CGRP is primarily expressed in the enteric nervous system and certain sensory neurons, contributing to gastrointestinal motility and local blood flow regulation (Russell et al., Physiological Reviews 2014). In clinical medicine, the CGRP pathway is a primary target for the treatment of migraine and cluster headaches, as elevated levels of the peptide are associated with the onset of attacks (Edvinsson, Nature Reviews Neurology 2017). Therapeutic interventions include monoclonal antibodies that specifically bind to the CGRP ligand, effectively neutralizing its biological activity and preventing the neurogenic inflammation and vasodilation that characterize migraine pathology (FDA Label: Emgality; FDA Label: Ajovy). Beyond its role in pain, β-CGRP is involved in cardiovascular homeostasis and may have protective effects in conditions like hypertension or ischemia (StatPearls: CGRP Inhibitors).

Other names
CALCBCalcitonin gene-related peptide 2CGRP-IICalcitonin gene-related peptide II
02

Mechanism of action

Monoclonal antibodies bind to the CGRP ligand (both alpha and beta isoforms), preventing it from activating the CGRP receptor complex (comprising CALCRL and RAMP1), thereby inhibiting vasodilation and pain signaling (Edvinsson, 2017; FDA Label: Emgality).

03

Biological functions

VasodilationNociceptionSensory neurotransmissionGastrointestinal motility regulation
04

Disease associations

MigraineCluster headacheChronic painInflammation
05

Safety considerations

ConstipationHypertensionHypersensitivity reactionsPotential impairment of compensatory vasodilation during ischemic events
06

Interacting drugs

Galcanezumab

2 more in the full profile.

07

Biomarkers

Elevated plasma CGRP levels during migraine attacksSalivary CGRP levels

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