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Obesity 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.