Drug intelligence / Profile preview

englitazone

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

Overview

Englitazone is a small molecule hypoglycemic agent of the thiazolidinedione (glitazone) class, developed as an experimental antidiabetic drug. It acts primarily as a peroxisome proliferator-activated receptor gamma (PPARγ) agonist, enhancing insulin sensitivity and exerting antihyperglycemic effects. In animal models and in vitro studies, englitazone lowers blood glucose, triglyceride, and cholesterol levels. Additional mechanisms include inhibition of ATP-sensitive potassium channels and calcium-activated non-selective cation channels in a voltage-independent manner. Englitazone also inhibits hepatic gluconeogenesis and glycogenolysis by activating cAMP phosphodiesterase and inhibiting Ca2+ influx in hepatocytes[1][2][3][4][5][6][7][8]. Developed by Pfizer, its primary indication was type 2 diabetes mellitus.

Other names
englitazonaEnglitazone [INN]
02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)

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