Drug intelligence / Profile preview

insulin + sitagliptin + metformin

Development stage
Phase 4
Lead developer
Merck
Modality
Small Molecules, Recombinant Proteins and Enzymes
Administration
Oral, Subcutaneous
01

Overview

This combination therapy for type 2 diabetes mellitus (T2DM) consists of three distinct anti-diabetic agents: insulin, sitagliptin, and metformin. **Insulin** is an exogenous hormone that facilitates peripheral glucose uptake and inhibits hepatic glucose production. **Sitagliptin** is a dipeptidyl peptidase 4 (DPP-4) inhibitor that increases the levels of active incretin hormones (GLP-1 and GIP), thereby stimulating insulin secretion and suppressing glucagon release in a glucose-dependent manner. **Metformin** is a biguanide that primarily reduces hepatic gluconeogenesis and improves insulin sensitivity. Research conducted by the Department of Endocrinology of the Affiliated Hospital of Jiangsu University has investigated this triple regimen's efficacy in stabilizing blood glucose fluctuations and preserving pancreatic beta-cell function in patients with T2DM who are inadequately controlled on standard therapies.

Other names
sitagliptin + metformin + insulininsulin, sitagliptin, and metformin combination
02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)DPP-4 (Dipeptidyl Peptidase-IV)INSR (Insulin receptor)GPD2 (Glycerol-3-phosphate dehydrogenase 2)

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