Delgocitinib is a specific Janus kinase (JAK) inhibitor. It demonstrates potent inhibitory activity against JAK1, JAK2, JAK3, and Tyk2 with IC50 values of 2.8, 2.6, 13, and 58 nM, respectively. It functions competitively with ATP and has shown effectiveness in suppressing various inflammatory responses both in vitro and in vivo.
- Inhibits all JAK subtypes.
- Competitively inhibits ATP binding to JAKs.
- Suppresses inflammatory responses.
- Reduces IFN-γ production.
- Prevents development of hind paw swelling and histological changes of inflammatory cell infiltration and synovial cell hyperplasia in relevant models.
- Inhibits radiographic and histological changes of bone and cartilage destruction in relevant models.
- Ameliorates inflammatory cell infiltration, synovial cell hyperplasia, and cartilage/bone destructions in histological and radiographic examinations.