Drug intelligence / Profile preview

glyburide + troglitazone

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of two oral antidiabetic agents, glyburide and troglitazone, used for the management of type 2 diabetes mellitus. Glyburide is a second-generation sulfonylurea that stimulates insulin secretion from pancreatic beta cells by closing ATP-sensitive potassium channels (sulfonylurea receptor 1), leading to increased intracellular calcium and subsequent insulin release. Troglitazone is a thiazolidinedione that acts as an agonist at peroxisome proliferator-activated receptor gamma (PPARγ), improving insulin sensitivity in peripheral tissues and reducing hepatic glucose output. The combination targets both impaired insulin secretion and insulin resistance, providing improved glycemic control compared to either agent alone. Troglitazone was withdrawn from the market due to concerns about hepatotoxicity but was previously developed by Warner-Lambert/Parke-Davis under the brand name Rezulin[1][3][5][6].

02

Targets

PPARA (Peroxisome proliferator-activated receptor alpha)PPARG (Peroxisome proliferator-activated receptor gamma)SUR1 (Sulfonylurea receptor 1)

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