saracatinib

Saracatinib is an orally available small molecule dual kinase inhibitor that selectively targets Src family kinases and Bcr-Abl tyrosine kinases. It was originally developed by AstraZeneca for the treatment of various cancers, including osteosarcoma, ovarian cancer, fallopian tube cancer, and primary peritoneal cancer. Saracatinib inhibits cell motility, migration, adhesion, invasion, proliferation, differentiation, and survival by blocking the activity of these kinases. Although it showed promising preclinical results and tolerability in early trials for cancer indications (with a maximum tolerated dose of 175 mg), phase II data revealed limited efficacy in oncology. The drug has since been repurposed for other diseases such as idiopathic pulmonary fibrosis (IPF), Alzheimer's disease (where it targets Fyn kinase), fibrodysplasia ossificans progressiva (as an ALK2 inhibitor), temporal lobe epilepsy (targeting Fyn/Src kinases), and schizophrenia. Saracatinib acts primarily through inhibition of Src family kinases—including c-Src and Fyn—as well as Abl kinase; it also potently inhibits ALK2/BMP type I receptor in certain contexts.

Other names

saracatinib