PF-04620110

PF-04620110 is a potent, selective, and orally bioavailable small molecule inhibitor of diacylglycerol acyltransferase 1 (DGAT-1), an enzyme that catalyzes the final step in triglyceride biosynthesis. By inhibiting DGAT-1 with high selectivity (IC50 = 19 nM), PF-04620110 reduces plasma triglyceride levels and suppresses fatty acid-induced NLRP3 inflammasome activation. It was developed by Pfizer for potential treatment of metabolic diseases such as type 2 diabetes and obesity. Preclinical studies demonstrated efficacy in lowering blood glucose and triglycerides in animal models, but clinical development was discontinued after phase I trials[1][4][5][8].