Orlistat is a reversible inhibitor of gastrointestinal lipases indicated for weight loss and weight maintenance. The global prevalence of obesity is increasing rapidly.
- Mechanism
- Curator reviewed · 2 references
Orlistat is a potent and selective inhibitor of various lipase enzymes responsible for the metabolism of fat. It acts in the gastrointestinal (GI) tract via covalent binding to the serine residues located on the active site of both gastric and pancreatic lipase. When orlistat is taken with food containing fat, it partially inhibits the hydrolysis of triglycerides. This decreases absorption of monoaclglycerides and free fatty acids, contributing to weight maintenance and weight loss.
- Primary indication
- Orlistat is indicated for obesity management including weight loss and weight maintenance when used in combination with calorie reduction in overweight and obese adults; this indication applies to both the prescription formulation of 120 mg...Curator reviewed · 3 structured indications
- Formula / weight
- C29H53NO5 · 495.7348 g/mol (avg)
- First approval
- Canada, 2017 · United States, 2007 · European Union, 2016
- Also known as
- Orlipastat · Tetrahydrolipstatin
- Code names
- RO 18-0647/002
- Brand names
Resolves to
AHLBNYSZXLDEJQ-FWEHEUNISA-NSMILESCCCCCCCCCCC[C@@H](C[C@@H]1OC(=O)[C@H]1CCCCCC)OC(=O)[C@H](CC(C)C)NC=OWhat you can answer from here — as of September 20, 2026
Which drugs share a target with Orlistat, and which of those have an active Phase 3 trial?
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