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NCX 1015

Development stage
Discontinued
Lead developer
NicOx Research Institute
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Subcutaneous (preclinical), Rectal
01

Overview

NCX 1015 is a nitric oxide-releasing derivative of prednisolone developed by NicOx for the treatment of inflammatory diseases such as inflammatory bowel disease (IBD), asthma, and rheumatoid arthritis. It is an experimental small molecule that combines the anti-inflammatory properties of prednisolone with a nitric oxide-donating moiety. Preclinical studies demonstrated that NCX 1015 has greater anti-inflammatory potency than prednisolone alone in models of colitis, arthritis, allergic inflammation, and spinal cord injury. Its mechanism involves inhibition of pro-inflammatory cytokines (such as IFN-γ and TNF-α), suppression of NF-κB/Rel A nuclear translocation in immune cells, reduction in myeloperoxidase activity and apoptosis after injury, and stimulation of IL-10 production leading to regulatory T cell induction. Despite promising preclinical results showing improved efficacy over prednisolone with potentially fewer side effects due to the NO component, clinical development was discontinued after early-phase trials for IBD and preclinical studies for asthma and rheumatoid arthritis[1][2][3][4][5][8].

Other names
NO-prednisolonenitro-prednisolone
02

Targets

GR (Glucocorticoid receptor)

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