Drug intelligence / Profile preview

rosiglitazone + alpha-lipoic acid

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Rosiglitazone + alpha-lipoic acid is a combination of two agents with distinct mechanisms relevant to metabolic disorders, particularly type 2 diabetes and its complications. Rosiglitazone is a thiazolidinedione class antidiabetic drug that acts as a highly selective agonist for the peroxisome proliferator-activated receptor gamma (PPARγ), improving insulin sensitivity in adipose tissue, skeletal muscle, and liver by regulating transcription of insulin-responsive genes involved in glucose production, transport, and utilization[2][6]. Alpha-lipoic acid is an endogenous antioxidant used both as a dietary supplement and therapeutic agent; it modulates glucose metabolism through antioxidant effects and by enhancing insulin sensitivity via activation of the insulin receptor cascade[1][3][8]. While both drugs have been studied individually for their roles in glycemic control and diabetic complications such as neuropathy, clinical evidence suggests that combining them does not provide significant additive benefit over monotherapy with either agent when used alongside intensive insulin therapy in newly diagnosed type 2 diabetes[4].

02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)

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