Drug intelligence / Profile preview

AZD1656 + sitagliptin

Development stage
Phase 1
Lead developer
Conduit Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

AZD1656 + sitagliptin is an experimental combination therapy investigated for potential use in patients with type 2 diabetes mellitus. AZD1656 is a small molecule glucokinase activator developed by AstraZeneca, designed to enhance the activity of glucokinase and thereby increase glucose uptake and metabolism in the liver and pancreas[1][2]. Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that elevates endogenous incretin levels, particularly glucagon-like peptide-1 (GLP-1), resulting in increased insulin secretion and reduced glucagon levels. Both agents are oral antidiabetic medications but operate through complementary mechanisms: AZD1656 promotes insulin secretion via direct glucokinase activation, while sitagliptin enhances incretin-mediated insulin secretion. Their combination is investigated to assess both pharmacokinetic interactions and their combined potential to improve glycemic control in type 2 diabetes[3][7].

02

Targets

DPP-4 (Dipeptidyl Peptidase-IV)GCK (Glucokinase)

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