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buprenorphine + naltrexone (UT Southwestern Medical Center)
- Development stage
- Phase 3
- Lead developer
- UT Southwestern Medical Center
- Modality
- Small Molecules
- Administration
- Subcutaneous, Intramuscular
01
Overview
This combination therapy consists of extended-release injectable buprenorphine (XR-BUP) and extended-release injectable naltrexone (XR-NTX), being evaluated by the University of Texas Southwestern Medical Center for the treatment of cocaine use disorder (CUD). The therapeutic rationale, often referred to as the 'kappa antagonist' strategy, utilizes buprenorphine's potent antagonism of the kappa opioid receptor (KOR) to mitigate the dysphoria and drug-seeking behavior associated with cocaine withdrawal. To prevent the potential for abuse or opioid-like effects from buprenorphine's mu opioid receptor (MOR) partial agonism, naltrexone is co-administered as a full MOR antagonist. The use of monthly extended-release injectable formulations (Sublocade for buprenorphine and Vivitrol for naltrexone) ensures medication adherence through directly observed therapy.
- Other names
- extended-release buprenorphine + extended-release naltrexoneXR-BUP + XR-NTXkappa antagonist combination
02
Targets
NOP (Nociceptin/orphanin FQ peptide receptor)DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)
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