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ContraveTM: novel treatment for obesity

Abstract The development of novel pharmacological agents capable of aiding weight loss is urgently required to help combat the global epidemic of obesity. ContraveTM is a fixed-dose combination of bupropion sustained release and naltrexone sustained release that is currently being examined in Phase III clinical trials as a potential new pharmacological treatment for obesity. Bupropion, a nonselective dopamine- and norepinephrine-reuptake inhibitor, is believed to reduce weight by stimulating hypothalamic proopiomelanocortin neurons, which in turn act to reduce appetite and increase energy expenditure, a mechanism that is inhibited by b-endorphin. Naltrexone, a ì-opioid receptor antagonist, acts in a synergistic manner with bupropion to induce weight loss, by blocking the b-endorphin-mediated inhibition of the proopiomelanocortin neuron. Preliminary results from ongoing Phase III clinical studies have recently reported that Contrave is both safe and efficacious as a pharmacological treatment for obesity, providing a potentially novel therapeutic strategy for its treatment. However, further rigorous clinical testing in nonselected patient populations will be required before this novel treatment strategy enters clinical use.