Lipid - Lowering Drugs Orlistat for Treatment of Obesity 96829-58-2

A New Type of Lipid - Lowering Drugs

Orlistat is a long-acting and potent specific inhibitor of gastrointestinal tract lipase, appearing as white or white-like powder at room temperature and being insoluble in water, soluble in chloroform and easily soluble in ethanol. It can form covalent bonds with the active serine sites of the gastric lipase and the pancreatic lipase in the stomach and small intestine cavity, resulting in inactivation of the enzymes. Fat in food can't be broken down into free fatty acids and monoacylglycerols so that the fat can't be absorbed and utilized, thereby having reduced the body's calorie intake to control the body weight.
The drug does not need to be absorbed through the body. At normal doses, the absorption of fat can be inhibited by 30%. There is little absorption after oral administration. It can be subject to metabolic inactivation in the intestine with the metabolic sites located in the gastrointestinal wall. The elimination half-life is about 14 to 19 hours. About 97% of the goods are excreted with the feces, of which 83% are in the prototype.
Clinically orlistat can be applied to the treatment of obesity and hyperlipidemia. Under normal circumstances, it can be subject to oral administration at a dose of 120 mg for three times per day. Take it during the meal or 1 hour after a meal. After 2 weeks of administration, the body weight can begin to decline. It can be taken continuously for 6 to 12 months. If the dose is increased to above 400 mg daily, the effect will no longer be further enhanced.


Orlistat Basic Information

Synonyms:(S)-2-Formylamino-4-Methyl-Pentanoic Acid (S)-1-[[(2s,3s)-3-Hexyl-4-Oxo-2-Oxetanyl]Methyl]-Dodecyl Ester;Xenical;Orlipastat
CAS:96829-58-2
MF:  C29H53NO5
MW:495.73
Chemical Properties: Off-White Solid
Usage: Tetrahydrolipstatin (orlistat) is a semi-synthetic derivative of lipstatin, a metabolite isolated from Streptomyces toxytricini. Tetrahydrolipstatin acts as a potent, irreversible inhibitor of pancreatic lipase. In vivo, it blocks the absorption of triglycerides while allowing fatty acid absorption. Tetrahydrolipstatin is widely used for the treatment of obesity.


Orlistat Specification