Drug intelligence / Profile preview

AC187

Development stage
Discontinued
Lead developer
Bristol Myers Squibb
Modality
Small Molecules, Peptides
Administration
Intraperitoneal, Intracerebroventricular, Subcutaneous, Intravenous
01

Overview

AC187 is a synthetic peptide and potent, selective amylin receptor antagonist. It exhibits high affinity for the amylin receptor (IC50 of 0.48 nM; Ki of 0.275 nM), with much greater selectivity over calcitonin and CGRP receptors[1][6]. Mechanistically, it competitively blocks the action of endogenous or exogenous amylin at its receptor sites[4]. Preclinical studies show that AC187 increases food intake in animal models by antagonizing the anorectic effects of amylin and has neuroprotective effects by blocking amyloid β-induced neurotoxicity[1][3][6]. It was initially developed by Bristol Myers Squibb/Saint Nazaire Assets for metabolic diseases such as diabetes mellitus but development was discontinued before clinical approval[2].

Other names
acetyl-(Asn30,Tyr32)-calcitonin8-32salmon calcitonin (8-32) reduced
02

Targets

AMY receptor (Calcitonin receptor (with ramps))

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