Tesaglitazar.: Treatment of type 2 diabetes, treatment of metabolic syndrome, PPARα/PPARγ agonist

Peroxisome proliferator-activated receptors (PPARs) modulate gene expression in the process of lipid metabolism. Tesaglitazar is a novel, dual PPAR agonist which binds to and activates both alpha and gamma receptor subtypes with similar high potency. It is currently being developed for the treatment of insulin resistance-related glucose and lipid abnormalities associated with type 2 diabetes and the metabolic syndrome. In rodent models of insulin resistance, tesaglitazar has been shown to improve insulin sensitivity and to have beneficial effects on fatty acid and glucose metabolism. In nondiabetic subjects with abnormalities characteristic of insulin resistance, there were significant dose-dependent reductions in fasting triglycerides, glucose and insulin in subjects treated with tesaglitazar. The drug is currently in phase III trials.