rebastinib

Rebastinib is an orally bioavailable small-molecule inhibitor of multiple tyrosine kinases, developed as an antineoplastic agent. Its mechanism of action involves inhibition of several key kinases, including Bcr-Abl tyrosine kinase (notably the T315I mutant), TIE2 receptor tyrosine kinase, Fms-like tyrosine kinase 3 (FLT3), VEGFR2, and members of the Src family such as Lyn protein tyrosine kinase and Proto-oncogene protein c-hck (HCK). Rebastinib acts as a "switch control" inhibitor by binding to a specific pocket in these kinases that locks them in their inactive conformation, thereby blocking downstream signaling pathways essential for cancer cell survival and proliferation. The drug has been investigated primarily for hematologic malignancies like chronic myeloid leukemia (CML) and acute myeloid leukemia (AML), as well as various solid tumors including breast cancer and ovarian cancer. Rebastinib was originally developed by Deciphera Pharmaceuticals (now acquired by Ono Pharmaceutical) and has undergone clinical trials but its development for all indications appears to have been discontinued[1][4][5][8].

Other names

rebastinib tosylate