How does Orlistat work?

April 2, 2021

Orlistat (also known as tetrahydrolipstatin) is a drug designed to treat obesity. It is marketed as a prescription drug under the trade name by Roche in most countries, and is sold over-the-counter as by GlaxoSmithKline in the United Kingdom and the United States.Its primary function is preventing the absorption of fats from the human diet by acting as a lipase inhibitor, thereby reducing caloric intake. It is intended for use in conjunction with a healthcare provider-supervised reduced-calorie diet.

Orlistat is the saturated derivative of lipstatin, a potent natural inhibitor of pancreatic lipases isolated from the bacterium Streptomyces toxytricini.However, due to its relative simplicity and stability, orlistat was chosen over lipstatin for development as an anti-obesity drug.

Orlistat is a semi-synthetic derivative of lipstatin , a metabolite isolated from Streptomyces toxytricini . Orlistat acts as a potent , irreversible inhibitor of pancreatic lipase . In vivo , it blocks the absorption of triglycerides while allowing fatty acid absorption .

Orlistat is widely used for the treatment of obesity as weight loss steroids .Biological Activity Hypolipemic pancreatic , gastric and carboxylester lipase inhibitor . Exhibits no activity at phospholipase A 2 , liver esterase , trypsin and chymotrypsin . Inhibits the thioesterase domain of fatty acid synthase , leading to cell cycle arrest at the G 1 /S boundary in vitro . Prevents the absorption of approximately one third of fat from food and exhibits pro-gastrokinetic , antiobesity and antihypercholesterolemic activity in vivo .