Drug intelligence / Profile preview

MK-4232

Development stage: Unknown
Lead developer: Merck
Modality: Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration: Intravenous

Overview

MK-4232 is a highly potent, central nervous system (CNS)-penetrant antagonist of the calcitonin gene-related peptide (CGRP) receptor. It was developed as a radiolabeled positron emission tomography (PET) tracer to visualize and quantify CGRP receptor distribution in the brain. The compound was derived from modifications of the CGRP receptor antagonist MK-3207 to enhance CNS penetrance and allow for radiolabeling with carbon-11. [(11)C]MK-4232 has been used in preclinical and clinical imaging studies to map CGRP receptors, which are implicated in migraine pathophysiology. The highest concentrations of binding were observed in the cerebellum and brainstem regions of both rhesus monkeys and humans[1][2][3][4][6].

Other names: [(11)C]MK-4232[11C]MK-42328Compound 8Compound8Compound-8

Targets

Calcitonin gene-related peptide type 1 receptor

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