Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor ( PPAR ) agonist with predominant PPARα and moderate PPARγ activity with EC 50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
In Vivo
In db/db mice, 12-day treatment with Saroglitazar (0.01-3 mg/kg per day, orally) causes dose-dependent reductions in serum triglycerides (TG), free fatty acids (FFA), and glucose. The ED 50 for these effects is found to be 0.05, 0.19, and 0.19 mg/kg, respectively with AUC-glucose following oral glucose administration (59%) at 1 mg/kg dose. A 90-day repeated dose comparative study in Wistar rats and marmosets confirms efficacy (TG lowering) potential of Saroglitazar and has indicated low risk of PPAR-associated side effects in humans. Based on efficacy and safety profile, Saroglitazar appears to have good potential as novel therapeutic agent for treatment of dyslipidemia and diabetes . MCE has not independently confirmed the accuracy of these methods. They are for reference only.