OTS964

OTS964 (and its analog OTS514) is a potent and selective small-molecule inhibitor of T-LAK cell-originated protein kinase (TOPK), also known as PBK (PDZ-binding kinase). Developed by Oncotherapy Science, it targets a serine/threonine protein kinase that is highly overexpressed in various human cancers—including small cell lung cancer, acute myeloid leukemia, kidney cancer, and glioblastoma—but is largely absent in normal adult tissues except the testis. The drug disrupts cancer cell division by inducing cytokinesis defects, which leads to apoptotic cell death and the suppression of cancer stem cell populations. Preclinical studies have demonstrated significant tumor regression, with a liposomal formulation of OTS964 achieving complete regression in lung cancer xenograft models when administered intravenously.

Other names

TOPK inhibitorPBK inhibitorPDZ-binding kinase inhibitor