"目录号: HY-13618
Cell Cycle/DNA Damage-
Edotecarin 是一种有效的topoisomerase I抑制剂，可诱导单链 DNA 断裂，IC50值为 50 nM。
Topoisomerase
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生物活性
Description
Edotecarin is a potent inhibitor oftopoisomerase Ithat can induces single-strand DNA cleavage, withIC50of 50 nM.
IC50& Target
IC50: 50 nM (topoisomerase I)[1]
In Vitro
In the presence of human colon cancer cells labeled with3Hthymidine, edotecarin (0.6 μmol/L) increases the formation of DNA-protein complexes in a time-dependent manner[1].
In Vivo
Edotecarin produces an 83% increase in survival in mice bearing intracranial D-456MG glioma and shows a strong antimetastatic effect[1]. Edotecarin results in tumor growth delays ranging from 10.45 days at the lowest dose (3 mg/kg) to 24.83 days at the highest (100 mg/kg). Combination treatment of edotecarin plus irinotecan improves antitumor activity in vivo compared with either agent alone[2].
Clinical Trial
NCT00087503
Pfizer
Stomach Neoplasms
April 2004
Phase 2
NCT00068952
Pfizer
Glioblastoma
August 2003
Phase 3
NCT00070031
Memorial Sloan Kettering Cancer Center-National Cancer Institute (NCI)
Breast Cancer
June 2003
Phase 2
NCT00072332
Memorial Sloan Kettering Cancer Center-National Cancer Institute (NCI)
Esophageal Cancer-Gastric Cancer-Unspecified Adult Solid Tumor, Protocol Specific
August 2003
Phase 1
NCT00067314
Pfizer
Breast Neoplasms-Neoplasm Metastasis
June 2003
Phase 2
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References
[1].Saif MW, et al. Edotecarin: a novel topoisomerase I inhibitor. Clin Colorectal Cancer. 2005 May;5(1):27-36.
[2].Ciomei M, et al. Antitumor efficacy of edotecarin as a single agent and in combination with chemotherapy agents in a xenograft model. Clin Cancer Res. 2006 May 1;12(9):2856-61.