Cetilistat powder 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. Cetilistat was shown to produce similar weight loss to orlistat.
|Molecular Weight||401.591 g/mol|
|Appearance||White to Off-White Powder|
|Half Life||Half-life of 9.4-16 h in humans, longer than those in rats (4.4 h) and fed dogs (7.3 h)|
|Solubility||Chloroform (Slighlty), Ethyl Acetate (Slightly)|
|Application||Investigated for use/treatment in obesity.|
Obesity powder is a modern plague in industrialized and developing countries, and currently overweight and obesity cause more deaths worldwide than underweight. Cetilistat is a novel, orally active, gastrointestinal and pancreatic lipase inhibitor. In in vitro studies cetilistat inhibited human pancreatic lipase with an IC50 in the low nanomolar range. In phase II clinical tials in obese patients and in obese patients with type 2 diabetes, cetilistat administered for 12 weeks significantly reduced body weight, serum low-density lipoprotein (LDL) cholesterol and total cholesterol in comparison to placebo. The proportion of obese patients reaching a reduction in baseline body weight of at least 5% was greater in all active arms in comparison to placebo. In obese diabetic patients the levels of glycosylated hemoglobin (HbA1c) were also significatively reduced. Cetilistat showed mild to moderate adverse events, predominantly of gastrointestinal nature (steatorrhea), with an incidence lower than orlistat. It was recently approved in Japan for the treatment of obesity with complications.
Developed by Alizyme, a specialist biopharmaceutical company in collaboration with Takeda Pharmaceutical, cetilistat (ATL-962) is an experimental treatment for obesity. Cetilistat restricts pancreatic lipases and acts as an agent to treat obesity and related diabetes or dyslipidemia.
It results in weight loss and absorbs fat from diet. The drug acts peripherally to reduce the appetite, without affecting the brain.
In December 2008, Takeda started a Phase III clinical study of cetilistat in Japan. Progress to pivotal Phase III trials followed encouraging Phase II clinical trial data that showed cetilistat promoted significant weight loss and was generally well tolerated in clinically obese patients.
Takeda evaluated European Phase II data of cetilistat in August 2003 and in January 2004 made an agreement with Alizyme to exclusively develop, manufacture and market cetilistat in Japan.
In October 2012, Takeda submitted a New Drug Application (NDA) for Cetilistat to Japan’s Ministry of Health, Labour and Welfare for the treatment of obesity.
Alizyme’s current research and development is focused on treatments for gastrointestinal disorders, obesity, cancer and diabetes.
Cetilistat is a gastrointestinal lipase inhibitor that blocks fat digestion and absorption, leading to reduced energy intake, and thus weight loss. It is distinct from most other anti-obesity agents as it does not act on the brain to reduce appetite, but acts peripherally. The compound remains in the gastrointestinal tract with no significant absorption into the body.
Cetilistat, under the brand name Cetislim, Checkwt, or Kilfat, is a new drug that is currently undergoing experimentation and clinical trials in various parts of the world for its effectiveness.
Cetilistat is classified under the “anti-obesity or anorectic drugs” category. Obesity happens to be one of the significant issues of modern times, mostly in developing and industrialized countries.
Cetilistat is an intra-orally active anti-obesity drug. It primarily functions as a gastrointestinal and pancreatic lipase inhibitor.
Cetilistat is used as a supplement to a healthy diet and exercise for a short term in the treatment of obesity. Cetilistat is also used for purposes that are not found in the medication guide.
Cetilistat is an experimental anti-obesity drug and is currently being researched on in Japan, the U.S, and Europe. Because Cetilistat is undergoing clinical trials, there is no efficacy or safety ensured as of yet for this drug.
In human trials, cetilistat was shown to produce similar weight loss to orlistat, but also produced similar side effects such as oily, loose stools, fecal incontinence, frequent bowel movements, and flatulence. It is likely that the same precautions would apply in that absorption of fat-soluble vitamins and other fat-soluble nutrients may be inhibited, requiring vitamin supplements to be used to avoid deficiencies.
Cetilistat has completed Phase 1 and 2 trials in the West and is currently in Phase 3 trials in Japan where it is partnered with Takeda. Norgina BV has now acquired the full global rights to cetilistat from Alizyme after the latter went into administration.
A published phase 2 trial found cetilistat significantly reduced weight with and was better tolerated than orlistat.