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Drug intelligence / Profile preview
naltrexone (Alkermes)
- Development stage
- Approved
- Lead developer
- Alkermes
- Modality
- Small Molecules
- Administration
- Intramuscular
01
Overview
Naltrexone is a long-acting opioid antagonist used primarily in the management of alcohol and opioid dependence. The depot formulation, often referred to as extended-release injectable naltrexone (XR-NTX), utilizes a polylactide-co-glycolide (PLGA) microsphere technology to provide therapeutic plasma concentrations for approximately one month following a single intramuscular injection. Its primary mechanism of action involves the competitive antagonism of mu-opioid receptors, which attenuates the reinforcing effects associated with alcohol consumption and reduces cravings. This formulation was specifically evaluated by the US Department of Veterans Affairs in studies involving homeless veterans to address the challenges of medication adherence and to support housing stability by reducing heavy drinking days. While Alkermes is the primary developer of the commercialized depot version (Vivitrol), the VA has played a significant role in clinical research for its application in high-risk veteran populations.
- Brand names
- Vivitrol
- Other names
- depot naltrexonenaltrexone extended-releaseXR-NTXnaltrexone depotnaltrexone extended-release injectable suspension
02
Targets
DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)
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