Saroglitazar Magnesium

Saroglitazar magnesium is a dual agonist of PPARα and PPARγ (EC₅₀s = 0.65 and 3,000 pM, respectively, in a transactivation assay in HepG2 cells).¹ It decreases serum triglyceride, free fatty acid, and glucose levels in a db/db mouse model of diabetes when administered at doses ranging from 0.01 to 3 mg/kg per day for 12 days. It increases insulin sensitivity in an oral glucose challenge when administered at a dose of 1 mg/kg in db/db mice, as well as decreases LDL levels in hApoB100/hCETP mice and in hamsters fed a high-fat high-cholesterol diet. Saroglitazar magnesium (10 µM) reverses palmitic acid-induced decreases in the expression of mRNA encoding superoxide dismutase 1 (SOD1), SOD2, glutathione peroxidase (GPX), and catalase and increases in the expression of mRNA encoding TNF-α, IL-1β, and IL-6 in HepG2 cells.² It decreases hepatic inflammation and steatosis in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a choline-deficient high-fat diet when administered at a dose of 3 mg/kg and inhibits hepatic fibrosis in a mouse model of fibrosis induced by carbon tetrachloride.

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1. Jain, M.R., Giri, S.R., Trivedi, C., et al. Saroglitazar, a novel PPARα/γ agonist with predominant PPARα activity, shows lipid-lowering and insulin-sensitizing effects in preclinical models. Pharmacol. Res. Perspect. 3(3), e00136 (2015).

2. Jain, M.R., Giri, S.R., Bhoi, B., et al. Dual PPARα/γ agonist saroglitazar improves liver histopathology and biochemistry in experimental NASH models. Liver Int. 38(6), 1084-1094 (2018).