orlistat

Orlistat is a small molecule drug used for the treatment of obesity. It acts as a potent and selective inhibitor of gastrointestinal lipases, specifically gastric and pancreatic lipase enzymes. By covalently binding to the serine residue at the active site of these enzymes, orlistat blocks the hydrolysis of dietary triglycerides into absorbable free fatty acids and monoglycerides, thereby reducing fat absorption by approximately 30% at therapeutic doses[5][6][8]. Orlistat is indicated for weight loss and weight maintenance in overweight adults, often in conjunction with a reduced-calorie diet and increased physical activity[1][3][4]. The drug was developed as a saturated derivative of lipstatin (originally isolated from Streptomyces toxytricini) due to its greater stability[5]. Orlistat has been shown to modestly reduce blood pressure and lower the risk of developing type 2 diabetes in obese individuals[5].

Brand names

AlliXenical

Other names

tetrahydrolipstatin