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2018年8月29日星期三

Cetilistat/Oblean®

↬ Basic Information

Cetilistat was jointly developed by Norgine and Takeda and was approved by the Japan Pharmaceutical and Medical Devices Integration Agency (PMDA) on September 20, 2013. It is marketed by Takeda in Japan under the trade name Oblean®. .

Celeste is a pancreatic lipase inhibitor that breaks down triglycerides in the intestines. Both Sylvester and the previous orlistat act by inhibiting pancreatic lipase. Without pancreatic lipase, triglycerides obtained from the diet are directly excreted because they cannot be hydrolyzed into absorbable free fatty acids. The drug is indicated for the treatment of obesity complications, limited to patients with both type 2 diabetes and dyslipidemia, and with a BMI greater than 25 kg/m2 despite undergoing controlled diet and exercise therapy.

Oblean® is an oral tablet containing 120 mg of celestatin per tablet. The recommended dose is 120mg each time, 3 times a day, and taken immediately after a meal.

↬ Structural formula



↬ Mechanism



Is a long-acting and potent specific gastrointestinal lipase inhibitor that inactivates enzymes by forming covalent bonds with the active serine sites of gastric and intestinal lumen gastric lipase and pancreatic lipase. In order to exert a therapeutic effect, the inactivated enzyme cannot hydrolyze the fat in the food, mainly triglyceride, into an absorbable free fatty acid and a monoacylglycerol. Undigested triglycerides are not absorbed by the body, reducing calorie intake and controlling body weight

↬ Synthetic route


↬ Research key data




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