AZD7687

AZD-7687 is a potent, selective, reversible, and orally active small molecule inhibitor of diacylglycerol O-acyltransferase 1 (DGAT1), an enzyme that catalyzes the final and only committed step in triacylglycerol (TAG) synthesis. By inhibiting DGAT1, AZD-7687 reduces postprandial triglyceride excursions and alters lipid handling and hormone secretion in the gut. It was developed by AstraZeneca for potential treatment of obesity and type 2 diabetes mellitus. Clinical studies demonstrated significant reductions in postprandial serum TAGs as well as increases in gut hormones such as GLP-1 and PYY; however, gastrointestinal side effects including diarrhea limited its therapeutic window. The drug reached phase 1 clinical trials but development was discontinued[1][3][4][5][6][7].