Obesity and overweight have become increasingly significant conditions, affecting more than 70% of the adult population in the United States. These conditions are caused by a combination of factors, including genetic, behavioral, environmental, and medical influences. Obesity is a major risk factor for cardiovascular and metabolic diseases. A comprehensive treatment plan for individuals with obesity must recognize the chronic nature of the condition and offer strategies for weight reduction and long-term cardiometabolic benefits. Over the past several decades, multiple therapeutic options have been implemented to address weight loss, appetite regulation, and caloric expenditure, with the goal of reducing the burden of obesity and improving cardiovascular outcomes. Pharmacological treatment of obesity has focused primarily on the central regulation of appetite and food intake behavior. The introduction of incretin agonists for obesity treatment has ushered in a new era of cardiometabolic health, with a multitargeted mechanism that achieves weight loss, glycemic control, decreased cardiovascular mortality, and other metabolic benefits. This review explores the current pharmacological options and the future of obesity treatment.