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naltrexone + bupropion
- Development stage
- Approved
- Lead developer
- Orexigen Therapeutics, Inc
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Naltrexone + bupropion is a fixed-dose combination medication used for weight management in obese or overweight adults with weight-related medical problems. It combines naltrexone, an opioid antagonist, and bupropion, an aminoketone antidepressant that acts as a norepinephrine/dopamine-reuptake inhibitor. The combination works by affecting areas of the brain involved in food intake regulation, including the hypothalamus (appetite regulation) and the mesolimbic dopamine circuit (reward pathways). The two components enhance the firing rate of hypothalamic pro-opiomelanocortin (POMC) neurons and block opioid receptor-mediated POMC auto-inhibition, leading to reduced food intake and increased energy expenditure. This medication is used in conjunction with a reduced-calorie diet and increased physical activity.
- Brand names
- ContraveMysimba
- Other names
- naltrexone HCl/bupropion HClnaltrexone hydrochloride/bupropion hydrochloride
02
Targets
NET (Norepinephrine Transporter)KOR (Kappa opioid receptor)Nicotinic Acetylcholine ReceptorDAT (Dopamine plasma membrane transport protein)MOR (Mu opioid receptor)DOR (Opioid Receptor Delta 1)
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