tozasertib

Tozasertib (MK-0457, VX-680) is a small molecule pan-Aurora kinase inhibitor that also exhibits activity against Flt-3 and Abl kinases. It was originally developed by Vertex and later by Merck. Tozasertib inhibits Aurora kinases A, B, and C, which are key regulators of mitosis and cell division. Inhibition of these kinases leads to G2-M cell cycle arrest, aneuploidy, apoptosis in cancer cells, and reduced tumor proliferation in preclinical models. The drug has been studied primarily for the treatment of advanced solid tumors and hematologic malignancies such as chronic myeloid leukemia (CML), acute myeloid leukemia (AML), ovarian cancer, colon cancer, pancreatic cancer, and clear cell renal cell carcinoma[2][4][5][7][10]. Clinical trials have shown some evidence of disease stabilization but development has not progressed beyond early-phase studies.

Other names

tozasertib lactate