Metabolic syndrome is a constellation of abnormalities, such as insulin resistance, central obesity, dyslipidemia, and high blood pressure. The definition and criteria for diagnosing metabolic syndrome keep changing and are a topic of debate. Regardless of the true criteria, the collection of these metabolic abnormalities increases the risk of developing type II diabetes mellitus and cardiovascular disease. The pathogenesis of metabolic syndrome involves the deregulation of various metabolic pathways involved in fatty acid metabolism, mitochondrial function, and glucose utilization. Metabolic syndrome is associated with an increased risk of other disorders, like nonalcoholic fatty liver, polycystic ovarian disease current terminology (PCOS), Alzheimer's disease, lipodystrophy, and Cushing's syndrome. The management of metabolic syndrome begins with lifestyle modification followed by pharmacotherapy of the individual component of metabolic syndrome. Weight reduction and lifestyle modification remains the mainstay of therapy of metabolic syndrome. Since insulin resistance is the major pathology behind the disease, insulin sensitizers, such as metformin and thiazolidinedione, are of great use. Hypolipidemic and antihypertensive drugs are used for treating other components of this syndrome. With the development in the field of molecular biology, the therapeutic targets for treating the individual components of the syndrome have been refined. This review focuses on the etiopathogenesis of metabolic syndrome and highlights the current and future therapeutic targets.