Cetilistat

Cetilistat

Cetilistat is a drug designed to treat obesity. It acts in the same way as the older drug orlistat (Xenical) by inhibiting pancreatic lipase, an enzyme that breaks down triglycerides in the intestine. Without this enzyme, triglycerides from the diet are prevented from being hydrolyzed into absorbable free fatty acids and are excreted undigested.

History

Cetilistat was developed by Alizyme, a biopharmaceutical company based in the United Kingdom. The drug was approved for the treatment of obesity in Japan by the Pharmaceuticals and Medical Devices Agency (PMDA) in September 2013. It is marketed in Japan by Takeda under the brand name Cetislim.

Mechanism of Action

Cetilistat works by inhibiting the action of pancreatic lipase, a lipolytic enzyme produced by the pancreas. This enzyme is responsible for the breakdown of triglycerides in the small intestine. When the activity of this enzyme is blocked, triglycerides from the diet are not hydrolyzed into absorbable free fatty acids, but are excreted in the feces. This reduces caloric intake and helps to decrease body weight.

Clinical Trials

In clinical trials, cetilistat was found to have similar efficacy to orlistat, but with fewer gastrointestinal side effects. In a phase 2 trial involving 612 obese patients, cetilistat significantly reduced body weight and was well-tolerated.

Side Effects

The most common side effects of cetilistat are gastrointestinal, including fatty or oily stool, increased defecation, and fecal incontinence. These side effects are generally mild and transient.

See Also

• Orlistat
• Pancreatic lipase
• Obesity