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Published on: June 9, 2017
NB-33, a bioreversible opioid derivative of Nalbuphine, shows enhanced pharmacodynamics
Michael Voronkov1, Georgiy Nikonov1, Roman Naumov1
1Kappa-Pharma LLC, 12085 Research Drive, Ste 156, Alachua, FL 32615, United States.
Abstract:
Developing non-addictive and safer opioids for pain management is unmet medical need. Among a number of bioreversible derivatives of Nalbuphine - an equipotent to morphine opioid without serious side effects - NB-33 was identified in silico and confirmed in vivo as a superior analgesic agent. Apart from enhanced pharmacodynamics profile, NB-33 outperformed the parent compound on equimolar bases in cold ethanol tail-flick and mechanical models of pain in rats. With no β-arrestin engagement liability, good stability in simulated gastro-intestinal fluid and slow release of Nalbuphine by plasma NB-33 is being developed as an oral and safer alternative of its parent drug.
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