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naltrexone + bupropion
- Development stage
- Approved
- Lead developer
- Currax Pharmaceuticals
- 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
DOR (Opioid Receptor Delta 1)DAT (Dopamine plasma membrane transport protein)KOR (Kappa opioid receptor)Nicotinic Acetylcholine ReceptorNET (Norepinephrine Transporter)MOR (Mu opioid receptor)
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