Orlistat

Excerpt

Orlistat (tetrahydrolipstatin) is an anti-obesity medication approved by the US Food and Drug Administration (FDA). This medication is a saturated derivative derived from the endogenous lipstatin found in Streptomyces toxytricini. Orlistat is used to manage obesity by reversibly inhibiting gastric and pancreatic lipases within the gut. These lipases play a crucial role in the digestion of dietary fat by breaking down triglycerides into absorbable free fatty acids and monoglycerides. Orlistat binds covalently to the serine residues of the active sites of these lipases, rendering them inactive. This inactivation of lipase prevents the hydrolysis of triglycerides, thereby impeding the absorption of free fatty acids.