Obesity has become the public health issue of the day—and for good reason. The data outline a dismal picture and a more foreboding future. The prevalence of obesity has doubled in adults and children and tripled in adolescents over the past 2 decades. Two thirds of Americans are overweight or obese. Each year in the United States, 400 000 deaths and $117 billion in health-care and related costs are attributable to obesity. Obesity is a complex, multi-factorial disease that develops from the interaction of genetic, social, behavioral, cultural, physiological, and metabolic factors. It is intimately linked to heart disease, sleep apnea, and certain cancers. Current main options for treatment of obesity including diet, physical exercise, behavioral therapy, and bariatric surgery have some degree of risk. Therefore, there is a strong need to develop a new effective and safe anti-obesity drug.Many pharmaceutical companies have invested substantial capital and labor to develop anti-obesity drugs; however, most of the anti-obesity drugs that have thus far been approved and marketed have ultimately been withdrawn because of their serious adverse effects. Scientists are trying to find and identify safe and effective anti-obesity bioactive ingredients from food or drugs, especially by inhibiting intestinal fat absorption, increasing fat cell metabolism, and enhancing the energy expenditure, such as lipase inhibitors, alpha-glucosidase inhibitors (αGI), and Maltase‐glucoamylase (MGA) inhibitors.

Traditional pharmacological monotherapies for obesity, although initially successful in achieving weight loss, are often subject to counter-regulation. This is not surprising given the multiplicity and redundancy of mechanisms involved in appetite regulation and energy homeostasis. It is therefore pertinent to note that combination agents that are designed to simultaneously target more than one biological mechanism might ultimately be more effective in producing sustained weight loss and improvements in comorbidities.

Based on the published literature, TargetMol carefully collects 2450 compounds with anti-obesity activity as Anti-Obesity Compound Library, which can be used for anti-obesity research and drug discovery.