Seladelpar

A potent, selective, orally bioavailable PPARδ agonist for the treatment of dyslipidemia, metabolic syndrome, type 2 diabetes, and non-alcoholic steatohepatitis (NASH) .Dyslipidemia Phase 2 Clinical (In Vitro) :MBX-8025 is an orally active, potent (EC50=2 nM), and specific (750-fold and 2500-fold compared with PPARα or PPARγ receptors, respectively) PPARδ agonist being developed as a lipid-altering agent. (In Vivo) :In atherogenic diet-fed Wt mice, administration of Seladelpar sodium salt reduces body weight by ~18% (P<0.05) . In contrast, Seladelpar sodium salt produces minimal effect on body weight in atherogenic diet-fed foz/foz mice. Seladelpar sodium salt lowers serum alanine aminotransferase (ALT) levels in foz/foz mice (P<0.05) and similarly (but not significantly) in Wt mice. Seladelpar sodium salt normalizes serum cholesterol and decreases triglycerides in both genotypes (P<0.05) . Seladelpar sodium salt abolishes hepatocyte ballooning (P<0.05) and decreases the nonalcoholic fatty liver disease (NAFLD) activity score by ~50%. Seladelpar sodium salt also significantly reduces sirius red-positive areas in foz/foz mice (P<0.05) .