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Drug nameOrlistat
DescriptionOrlistat is a drug designed to treat obesity. Its primary function is preventing the absorption of fats from the human diet, thereby reducing caloric intake. Orlistat works by inhibiting pancreatic lipase, an enzyme that breaks down triglycerides in the intestine. Without this enzyme, triglycerides from the diet are prevented from being hydrolyzed into absorbable free fatty acids and are excreted undigested.
DrugBankPrimary Accession Number: DB01083
TypeApproved, Investigational, Small Molecule
IndicationFor obesity management including weight loss and weight maintenance when used in conjunction with a reduced-calorie diet. Also used to reduce the risk for weight regain after prior weight loss.
Mechanism of ActionOrlistat is a reversible inhibitor of lipases. It exerts its therapeutic activity in the lumen of the stomach and small intestine by forming a covalent bond with the active serine residue site of gastric and pancreatic lipases. The inactivated enzymes are thus unavailable to hydrolyze dietary fat in the form of triglycerides into absorbable free fatty acids and monoglycerides. As undigested triglycerides are not absorbed, the resulting caloric deficit may have a positive effect on weight control.
AbsorptionSystemic absorption of orlistat is minimal, however systemic absorption of the drug is not needed for activity.
ToxicityThe results of a massive overdose of Xenical are unknown, although the drug seems relatively harmless.
Protein Binding>99% bound to plasma proteins (lipoproteins and albumin were major binding proteins).