Withdrawn 49th Annual Scientific Meeting of the Australian and New Zealand Society for Immunology 2021

Nalfurafine reduces neuroinflammation and drives remyelination in the CNS during demyelinating disease (#219)

Lisa Denny 1 2 , Afnan Al Abadey 1 2 , Katharina Robichon 1 2 , Nikki Templeton 1 2 , Thomas E Prisinzano 3 , Bronwyn M Kivell 1 2 , Anne C La Flamme 1 2 4
  1. Victoria University of Wellington, Wellington, New Zealand
  2. Centre for Biodiscovery, Victoria University of Wellington, Wellington, New Zealand
  3. Department of Pharmaceutical Sciences, University of Kentucky, Lexington, KY, USA
  4. Malaghan Institute of Medical Research, Wellington, New Zealand

Multiple sclerosis (MS) is a neurodegenerative disease characterized by immune-mediated damage to the myelin sheath resulting in physical and cognitive disability. While current treatments are effective at reducing disease relapse, there are no treatments available that prevent disease progression. Recent studies have reported that activating the kappa opioid receptors (KOR) with the KOR agonist, U50,488, is beneficial in a mouse model of MS, experimental autoimmune encephalomyelitis (EAE). Unfortunately, U50,488 is not suitable for clinical use due to its poor side-effect profile. However, we have found that nalfurafine, a potent and well-tolerated KOR agonist, which is in clinical use, enabled full recovery, enhanced remyelination, and reduced neuroinflammation in EAE when administered therapeutically (i.e. after disease onset). Additionally, nalfurafine was more effective than U50,488 and mediated full recovery from EAE in a KOR-dependent fashion. Finally, nalfurafine promoted remyelination in the cuprizone model of non-immune demyelination, supporting the direct effect on remyelination in the absence of peripheral immune cell invasion. Overall, our findings support the potential of nalfurafine to promote recovery and remyelination and highlight its promise for clinical use in MS.