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Cetilistat is a medicine used to treat obesity. It works the same way as the older drug orlistat (Xenical), by inhibiting pancreatic lipase, an enzyme that breaks down triglycerides in the gut. Without this enzyme, dietary triglycerides cannot be hydrolyzed into absorbable free fatty acids and are excreted undigested. 

In human trials, cetinostat showed similar weight loss effects as orlistat, but also produced similar side effects, such as greasy, loose stools, fecal incontinence, frequent bowel movements, and flatulence. The same precautions are likely to apply to fat-soluble vitamins and the absorption of other fat-soluble nutrients may be inhibited, requiring vitamin supplementation to avoid deficiencies.

Cetilistat has completed Phase 1 and 2 trials in the West and is currently in a Phase 3 trial in Japan in collaboration with Takeda Norgina BV acquired full global rights to cetilistat after Alizyme entered administration.

A published phase 2 trial found that cetilistat significantly reduced body weight and was better tolerated than orlistat.


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