Drug intelligence / Profile preview

troglitazone

Development stage
Phase 3
Lead developer
Daiichi Sankyo
Modality
Small Molecules
Administration
Oral
01

Overview

Troglitazone is an oral antidiabetic drug of the thiazolidinedione class that was used to treat type 2 diabetes mellitus. It lowers blood glucose by improving target cell response to insulin and acts primarily by decreasing insulin resistance in muscle and adipose tissue while inhibiting hepatic gluconeogenesis. Troglitazone’s mechanism of action involves binding to nuclear receptors peroxisome proliferator-activated receptor gamma (PPARγ) and also PPARα, with a higher affinity for PPARγ. This activation regulates transcription of genes involved in glucose and lipid metabolism. Troglitazone contains an α-tocopherol (vitamin E) moiety, potentially conferring additional antioxidant properties. The drug was developed by Sankyo and marketed as Rezulin by Pfizer but was withdrawn from the market due to hepatotoxicity concerns[1][2][3][4][6].

Brand names
RezulinPrelayRonglitazone
Other names
97322-87-7
02

Targets

TRPV1 (Transient receptor potential cation channel subfamily V member 1)PPARA (Peroxisome proliferator-activated receptor alpha)PPARG (Peroxisome proliferator-activated receptor gamma)

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