Individuals who are overweight or obese are at risk for multiple comorbidities (eg, hypertension, dyslipidemia, type 2 diabetes, coronary artery disease). Pharmacotherapy combined with lifestyle modification, energy restriction, and increased physical activity has been suggested as a potential treatment option for overweight or obese individuals. Orlistat, one pharmacological treatment option, inhibits pancreatic and gastric lipase activity. It is available both as a prescription drug (120 mg taken 3 times per day with meals) and as an over-the-counter drug (60 mg taken 3 times per day with meals). The efficacy of orlistat 60 mg for weight loss in overweight and obese individuals is addressed in this article. A case study is also presented, which explores orlistat 60 mg use in a 31-year-old obese man, with emphasis on efficacy, compliance, and adverse effects.