Orlistat

Hypolipemic cell permeable and irreversible pancreatic, gastric and carboxylester lipase inhibitor [1-3]. Anti-obesity and antihypercholesterolemic compound [2, 5, 11]. Antitumor compound by inhibition of the thioesterase domain of fatty acid synthase (FASN) [4, 6, 9, 10]. Anti-proliferative [4, 6, 9, 10]. Causes cell cycle arrest at G1 phase. Apoptosis inducer through caspase-3 activation [6, 10]. Sn-1-selective-diacylglycerol lipases alpha (DAGLalpha) inhibitor. Targets serine hydrolases in the nervous system, such as diacylglycerol lipase (DAGL), which is responsible for the conversion of DAG to 2-AG [7]. Partially inhibits the hydrolysis of triglycerides and lowers the absorption of dietary fat, promoting weight loss [8]. Promotes the sensitivity to TRAIL in cancer cells by ROS-mediated pathways [11].