CR10049

CR10049 is a small molecule multi-kinase inhibitor developed by Rottapharm Biotech for the treatment of the inflammatory phenotype of osteoarthritis (OA). Administered via intra-articular injection, it is designed as a long-acting symptom- and disease-modifying drug. CR10049 preferentially inhibits pro-inflammatory members of the Src family kinases (SFKs), including cSrc, Lck, Fyn, Fgr, Frk, and Yes, with nanomolar potency (IC50 < 25 nM). It also targets other kinases critical to OA progression, such as VEGFR1/2, FGFR1, EPHA3, EPHA5, TrkB, and TrkC. By targeting these pathways, the drug aims to mitigate synovial inflammation, fibrosis, cartilage degradation, bone remodeling, and pain. Preclinical animal models have demonstrated its potential for long-acting pain reduction and joint structure preservation.