plogosertib

Plogosertib (CYC140) is a novel, selective, and potent small molecule inhibitor of polo-like kinase 1 (PLK1), a serine/threonine kinase that plays a central role in cell division and regulation of the DNA damage checkpoint. Overexpression of PLK1 is associated with poor prognosis in several cancers. Plogosertib competitively inhibits ATP binding to PLK1, leading to mitotic arrest and apoptotic death in cancer cells while sparing normal cells with intact checkpoints. It has demonstrated antitumor activity in preclinical models across various tumor types including esophageal cancer and acute leukemia. Clinical development is ongoing for advanced solid tumors, leukemias, lymphomas, myelodysplastic syndrome (MDS), and metastatic colorectal cancer (including KRAS-mutated subtypes). The drug was designed for improved pharmaceutical properties over earlier PLK inhibitors[1][4][5][7].

Other names

PLK1 inhibitor CYC140PLK-1 inhibitor CYC140PLK 1 inhibitor CYC140