Ligand id: 5277

Name: orlistat

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View more information in the IUPHAR Pharmacology Education Project: orlistat

Structure and Physico-chemical Properties

2D Structure
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Calculated Physico-chemical Properties
Hydrogen bond acceptors 6
Hydrogen bond donors 1
Rotatable bonds 24
Topological polar surface area 81.7
Molecular weight 495.39
XLogP 10.26
No. Lipinski's rules broken 2

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Preventing the absorption of fats from the human diet, thereby reducing caloric intake in obesity. Orlistat is available form pharmacies without a prescription (OTC) in a number of countries, including the United States, European Union member states, and Australia. The OTC formulations are generally supplied in lower doses than those available on prescription.
Mechanism Of Action and Pharmacodynamic Effects
The primary effect of orlistat is local lipase inhibition within the GI tract. The enzymes are inhibited by drug interaction with serine residues within the enzymes' active sites. This renders the target enzymes unable to hydrolyse dietary triglyceride (fat) substrates into absorbable free fatty acids and monoglycerides, and the fats are excreted unchanged.
The primary route of elimination is through the feces.
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