Obesity is defined as overaccumulation of white adipose tissue in the body, mainly under the skin (subcutaneous adiposity) or in the abdominal cavity (visceral adiposity). It could be the origin of various metabolic disorders including hypertension, hyperlipidemia, type 2 diabetes, cardiovascular diseases etc. Active adipose tissue was discovered in humans through F-18-fluorodeoxyglucose Positron Emission Tomography coupled with Computer Tomography (F-18 FDG-PET/CT), which was initially performed for tumor scanning. Since human active adipose tissue is probably composed of brown and beige adipose tissues and they burn white adipose tissue to generate heat, targeting human brown/beige adipose tissue to induce their thermogenic function is considered significant to combat obesity. In this review, we describe the latest advancements on promising therapeutic strategies to combat obesity by targeting human thermogenic adipose tissues to achieve further metabolic balance in humans.