Oxytocin, initially recognized as a hormone that plays a key role in lactation and uterine contraction, has been recently discovered for its actions in the brain, assisting in the regulation of social and metabolic psychological behaviors. In light of metabolic control, Oxytocin is shown to induce feeding restriction and weight reduction by signaling the hypothalamus, the section of the brain responsible for hormone production, body temperature, thirst, hunger, sleep, mood and sex drive. Recent studies suggest that Oxytocin may also play a significant role in glucose metabolism, as well as insulin secretion and lipolysis. In addition, Oxytocin nasal spray has been proven effective in successfully inducing weight loss and metabolic improvement in obese patients. These studies and recent advances suggest a promising foundation for the therapeutic strategy of developing innovative Oxytocin peptidyl drugs for the treatment of obesity and related metabolic diseases.