Abstract: Obesity is a chronic metabolic disease caused by the excess of energy in body. It may lead to the type II diabetes, cardiovascular disease, hypertension, stroke, and a variety of cancers. At present, many drugs are using for the treatment of obesity. Gastrointestinal lipase inhibitors are the most effective drugs of that. This paper reviewed the research progress of the gastrointestinal lipase inhibitors in the treatment of obesity and its representative drug orlistat, which aimed to provide references for the development of slimming drugs.