Drug intelligence / Profile preview

DA-1241 + metformin

Development stage
Unknown
Lead developer
MetaVia
Modality
Small Molecules
Administration
Oral
01

Overview

DA-1241 + metformin is an investigational combination of DA-1241, a **novel small molecule agonist of G protein-coupled receptor 119 (GPR119)**, and **metformin**, a first-line biguanide hypoglycemic agent, under clinical evaluation primarily for the treatment of **type 2 diabetes mellitus**. DA-1241 stimulates GPR119 in the gut, promoting the release of gut hormones including **glucagon-like peptide-1 (GLP-1)**, glucose-dependent insulinotropic polypeptide (GIP), and peptide YY (PYY), leading to improved glycemic control via enhancement of glucose-dependent insulin secretion and inhibition of hepatic gluconeogenesis, potentially via modulation of autophagic flux in hepatocytes. Metformin acts primarily by reducing hepatic glucose production and improving insulin sensitivity. The combination is investigated for additive or synergistic effects on glycemic control and potential benefits for associated metabolic and hepatic conditions, including non-alcoholic steatohepatitis (NASH/MASH). Clinical studies indicate that DA-1241 in combination with metformin is well tolerated and provides clinically meaningful improvements in glycemic biomarkers in patients with type 2 diabetes mellitus[1][2][5].

02

Targets

GPR119 (Glucose-dependent insulinotropic receptor)AMPK (Adenosine monophosphate–activated protein kinase)

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