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Ximingtecan is a novel, water-soluble camptothecin derivative developed by the Shanghai Institute of Materia Medica (SIMM) of the Chinese Academy of Sciences. As a member of the camptothecin family, it functions as a DNA topoisomerase I inhibitor. The drug works by binding to and stabilizing the transient covalent complex formed between the topoisomerase I enzyme and DNA. This stabilization prevents the religation of the DNA strand, leading to the formation of permanent double-strand breaks when the replication fork encounters the complex during the S-phase of the cell cycle. These breaks trigger cell cycle arrest and apoptosis in rapidly dividing cancer cells. Ximingtecan has been investigated in Phase I clinical trials in China for the treatment of advanced solid tumors and metastatic colorectal cancer, both as a monotherapy and in combination with 5-fluorouracil and leucovorin.
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