Overweight and obesity, if sustained, are serious medical problems reaching an epidemic proportion. It is estimated that over 55% of the adult population is affected by overweight and obesity. Both overweight and obesity put these individuals at a high risk for the development of insulin resistance, hypertension, dyslipidemia, type 2 diabetes and coronary heart disease. A weight loss of between 5% and 10% of the initial body weight has been shown to greatly reduce these health risks associated with overweight and obesity. Typically, the first-line clinical strategy for weight loss is a combination of supervised diet, exercise and behavior modification. Although life style modification can exert beneficial effects in overweighed and obese individuals, it is difficult to achieve and maintain weight losses solely by life style change. Anti-obesity drugs may be used in obese patients (BMI of 30 or greater), or overweight patients with established comorbidities (BMI > 27), where dietary and lifestyle modifications are unsuccessful in achieving a 10% weight reduction following at least three months of the supervised care. Current anti-obesity drug therapy is geared towards reducing energy/food intake via actions on either gastrointestinal system or the central control of appetite and feeding. A thorough understanding of the molecular pathways involved in weight gain and appetite suppression should help for a better drug design and development. This mini review will focus on the molecular mechanisms and currently available pharmacotherapeutic interventions in overweight and obesity.