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Cetilistat is a small molecule drug that acts as a gastrointestinal and pancreatic lipase inhibitor. By inhibiting pancreatic lipase, an enzyme responsible for breaking down dietary triglycerides in the intestine, cetilistat prevents the hydrolysis of triglycerides into absorbable free fatty acids. As a result, undigested fats are excreted in the feces, leading to reduced fat absorption and caloric intake. This mechanism promotes weight loss and improves metabolic parameters such as HbA1c and LDL cholesterol in obese patients with or without type 2 diabetes. Unlike centrally acting anti-obesity agents, cetilistat works peripherally within the gastrointestinal tract with minimal systemic absorption[1][3][4][5]. It was originally developed by Alizyme and later by Norgine; Takeda marketed it as Oblean in Japan for obesity treatment[6].
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