Drug intelligence / Profile preview

DPP4 inhibitor + SGLT2 inhibitor + sulfonylurea

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

Overview

A combination therapy consisting of a **DPP4 inhibitor, an SGLT2 inhibitor, and a sulfonylurea** is used for the management of type 2 diabetes mellitus (T2DM) in patients who require additional glycemic control beyond monotherapy or dual therapy. - **DPP4 inhibitors** (dipeptidyl peptidase-4 inhibitors) enhance incretin levels, leading to increased insulin secretion and decreased glucagon secretion in a glucose-dependent manner. - **SGLT2 inhibitors** (sodium-glucose cotransporter 2 inhibitors) reduce blood glucose by increasing renal excretion of glucose, independent of insulin secretion or sensitivity. - **Sulfonylureas** stimulate pancreatic beta cells to increase endogenous insulin secretion. This triple oral antihyperglycemic regimen targets multiple pathophysiological defects in T2DM and is typically reserved for patients for whom other regimens (such as those including metformin) are inadequate or contraindicated. The regimen carries a higher risk of hypoglycemia compared to DPP4 inhibitor + SGLT2 inhibitor dual therapy, primarily due to the sulfonylurea component[1][2][5]. No fixed-dose combination product containing all three classes (DPP4 inhibitor + SGLT2 inhibitor + sulfonylurea) is currently marketed; therapy is generally administered as concurrent use of the individual agents.

02

Targets

DPP-4 (Dipeptidyl Peptidase-IV)KATP channel (ATP-sensitive potassium channel)SGLT2 (Sodium-glucose cotransporter protein subunit 2)

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