Drug intelligence / Profile preview

metformin + glimepiride + sitagliptin

Development stage
Unknown
Lead developer
Korea University Anam Hospital
Modality
Small Molecules
Administration
Oral
01

Overview

This refers to the conventional stepwise add-on treatment regimen used as a comparator in a clinical trial led by Korea University Anam Hospital for drug-naïve patients with type 2 diabetes mellitus. The regimen involves the sequential addition of glucose-lowering agents: starting with metformin monotherapy, followed by the addition of the sulfonylurea glimepiride, and finally the addition of the dipeptidyl-peptidase-4 (DPP-4) inhibitor sitagliptin. This approach follows traditional treatment algorithms where therapy is intensified only after failing to maintain glycemic targets with existing medications. Metformin works by reducing hepatic glucose production and improving insulin sensitivity; glimepiride, a second-generation sulfonylurea, stimulates insulin secretion from pancreatic beta cells by binding to the sulfonylurea receptor 1 (SUR1); and sitagliptin increases incretin levels to enhance glucose-dependent insulin secretion.

Other names
stepwise add-on therapy-Korea University Anam Hospital-type 2 diabetes mellitusStepwise add-on therapymetformin -> glimepiride -> sitagliptin
02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)ND1 (Mitochondrial electron transport chain complex I)OCT1 (Organic cation transporter 1)

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