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Umonsertib (LH011) is a small molecule inhibitor of Polo-like kinase 1 (PLK1), a serine/threonine kinase that plays a critical role in regulating mitosis. PLK1 is frequently overexpressed in various cancers and is associated with poor prognosis. By inhibiting PLK1, umonsertib interferes with centrosome maturation, bipolar spindle formation, and chromosome segregation, ultimately triggering mitotic catastrophe and apoptosis. Developed by Yuekang Pharmaceutical Group, umonsertib is being evaluated in Phase 1 clinical trials in China for the treatment of advanced solid tumors, including pancreatic cancer, where it is being studied as a monotherapy and in combination with gemcitabine.
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