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buprenorphine + naltrexone
- Development stage
- Unknown
- Lead developer
- Indivior
- Modality
- Small Molecules
- Administration
- Sublingual, Oral, Intramuscular, Subcutaneous
01
Overview
Buprenorphine + naltrexone is an experimental combination drug formulation consisting of buprenorphine, a partial agonist at the μ-opioid receptor (MOR) and antagonist at the κ-opioid receptor (KOR), and naltrexone, a silent antagonist at both MOR and KOR. This combination is under investigation for the treatment of psychiatric disorders, including substance use disorders such as cocaine dependence. The rationale behind this combination is to selectively block KOR while minimizing MOR activation-related effects like euphoria and opioid dependence. Preclinical studies have shown antidepressant-like effects in animal models, and clinical trials suggest efficacy in treating cocaine dependence[1].
- Brand names
- SubutexVivitrolBuprenex
- Other names
- buprenorphine/naltrexone
02
Targets
MOR (Mu opioid receptor)KOR (Kappa opioid receptor)
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