Drug intelligence / Profile preview

metformin + sitagliptin + repaglinide

Development stage
Preclinical
Lead developer
Novo Nordisk
Modality
Small Molecules
Administration
Oral
01

Overview

This is a hypothetical or investigational oral combination therapy consisting of three antidiabetic agents—metformin, sitagliptin, and repaglinide. Each component has a distinct mechanism of action for the management of type 2 diabetes mellitus: - **Metformin** is a biguanide that decreases hepatic glucose production, reduces intestinal absorption of glucose, and improves insulin sensitivity. - **Sitagliptin** is a dipeptidyl peptidase-4 (DPP-4) inhibitor that increases incretin levels (GLP-1 and GIP), thereby enhancing glucose-dependent insulin secretion and suppressing glucagon release. - **Repaglinide** is a meglitinide analog that stimulates rapid, short-duration insulin secretion from pancreatic beta cells in response to meals. While two-drug combinations such as metformin plus sitagliptin (Janumet) or metformin plus repaglinide (PrandiMet) are approved for type 2 diabetes[1][2][6][7], there are currently no marketed products or clinical evidence supporting the use of all three agents together in one fixed-dose combination. The rationale for combining these drugs would be to target multiple pathophysiological defects in type 2 diabetes with complementary mechanisms.

02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)DPP-4 (Dipeptidyl Peptidase-IV)SUR1 (Sulfonylurea receptor 1)

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