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xinotecan
- Development stage
- Phase 1
- Lead developer
- Shanghai Institute of Materia Medica
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
Xinotecan is a novel, water-soluble camptothecin derivative developed by the Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences. It functions as a DNA topoisomerase I inhibitor, a mechanism shared with other "tecan" drugs like irinotecan and topotecan. By stabilizing the covalent complex between DNA and the topoisomerase I enzyme (the "cleavable complex"), xinotecan prevents DNA religation, leading to lethal double-strand breaks during the S-phase of the cell cycle and subsequent apoptosis. The drug was designed to optimize the pharmacokinetic profile and reduce the toxicity associated with earlier camptothecin analogs. It has been evaluated in Phase 1 clinical trials in China for patients with advanced malignant solid tumors who have failed standard therapies.
- Other names
- 喜诺替康
02
Targets
TOP1 (DNA Topoisomerase I)
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