Drug intelligence / Profile preview

AC164209

Development stage
Discontinued
Lead developer
Bristol Myers Squibb
Modality
Small Molecules, Fc-Fusion Proteins → Carrier/Scaffold Proteins → Recombinant Proteins and Enzymes, Peptides
Administration
Subcutaneous
01

Overview

AC164209 is a synthetic peptide-based drug candidate developed as a dual agonist targeting both the glucagon-like peptide-1 (GLP-1) receptor and the amylin (islet amyloid polypeptide) pathway. It is classified as a "phybrid"—a single molecular entity that combines pharmacophores from both a GLP-1 receptor agonist and an amylin analog (specifically davalintide), linked via a β-Ala–β-Ala moiety. The drug was designed to harness the glucose-lowering effects of incretin therapy with enhanced weight loss properties compared to monotherapy with either parent compound. In preclinical studies in obese diabetic rodents, AC164209 improved glucose tolerance and reduced HbA1c levels while inducing greater body weight loss than exenatide or davalintide alone. Its mechanism of action involves dual activation of the GLP-1 receptor (stimulating insulin secretion and reducing appetite) and amylin receptors (regulating satiety and gastric emptying). Development was primarily aimed at treating metabolic diseases such as type 2 diabetes mellitus and obesity[2][5][6].

Other names
Amylinomimetic/GRA peptide hybridGLP-1 receptor agonist/amylin analogue hybridGLP-1 receptor agonist/amylin mimetic hybridGLP-1 receptor agonist/amylinomimetic hybridGRA/amylinomimetic peptide hybridINTO
02

Targets

GLP1R (GLP-1R)AMY receptor (Calcitonin receptor (with ramps))

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