Aleglitazar, a new, potent, and balanced dual PPARα/γ agonist for the treatment of type II diabetes

Abstract Design, synthesis, and SAR of novel α-alkoxy-β-arylpropionic acids as potent and balanced PPARαγ coagonists are described. One representative thereof, Aleglitazar ( (S) - 2Aa ), was chosen for clinical development. Its X-ray structure in complex with both receptors as well as its high efficacy in animal models of T2D and dyslipidemia are also presented.