Early Development of Ocadusertib, a Selective Receptor-Interacting Serine/Threonine-Protein Kinase 1 Inhibitor - PubMed
4 days ago
- #inflammatory diseases
- #RIPK1 inhibitor
- #clinical trials
- Ocadusertib is a selective allosteric inhibitor of RIPK1, being studied for chronic inflammatory diseases like rheumatoid arthritis, IBD, and psoriasis.
- Preclinical studies showed ocadusertib's high potency (IC50 = 12-38 nM) and selectivity for RIPK1, with no significant inhibition of over 100 other kinases.
- In mouse models, ocadusertib prevented RIPK1-dependent hypothermia and reduced disease severity in chronic proliferative dermatitis.
- Phase 1 trials in healthy participants demonstrated linear pharmacokinetics, dose-proportional exposure, and good tolerability with no serious adverse events.
- Target engagement studies showed >90% RIPK1 inhibition at Day 14, supporting further clinical evaluation for chronic inflammatory diseases.