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nalmefene prodrug
- Development stage
- Phase 1
- Lead developer
- Nirsum Laboratories
- Modality
- Small Molecules
- Administration
- Injectable
01
Overview
NRS-033 is a second-generation, long-acting injectable opioid antagonist developed by Nirsum Labs for the treatment of opioid use disorder (OUD) and alcohol use disorder (AUD). It is a small molecule drug and functions as a prodrug of nalmefene, designed to improve therapeutic retention compared to existing therapies. The drug acts as an opioid receptor antagonist, blocking the effects of opioids at their receptors. As of early 2025, NRS-033 has completed Phase I clinical trials in the United States for opioid-related disorders and is entering Phase II development for both OUD and AUD. The product aims to address high relapse rates associated with current treatments by providing longer-lasting antagonism[1][3][4][8].
- Other names
- NRS 033NRS033NRS-033
02
Targets
KOR (Kappa opioid receptor)DOR (Opioid Receptor Delta 1)MOR (Mu opioid receptor)
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