生物活性

• 描述Irinotecan is activated to SN-38 by carboxylesterases to become able to interact with its target, topoisomerase I. Irinotecan induces similar amounts of cleavable complexes at its IC50 in LoVo cells and HT-29 cell lines. SN-38 induces a concentration-dependent formation of cleavable complexes, which is not significantly different in LoVo cells and HT-29 cell lines. Cell accumulation of Irinotecan is markedly different, reaching consistently higher levels in HT-29 cells than in LoVo cells. The lactone E-ring of Irinotecan and SN-38 hydrolyses reversibly in aqueous solutions, and the interconversion between the lactone and carboxylate forms is dependent on pH and temperature. Liver is primarily responsible for the activation of Irinotecan to SN-38. At equal concentrations of Irinotecan and SN-38 glucuronide, the rate of beta-glucuronidase-mediated SN-38 production is higher than that formed from Irinotecan in both tumour and normal tissue. Irinotecan is also converted to SN-38 in intestines, plasma and tumor tissues. Irinotecan is significantly more active in SCLC than in NSCLC cell lines, whereas no significant difference between histological types is observed with SN-38.
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00483834	Colorectal Cancer	Phase 2	Completed	-	Canada, Ontario ... more >> Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Collapse <<
  NCT03245450	Refractory or Recurrent Solid ... more >>Tumors Rhabdomyosarcoma Non-Rhabdomyosarcoma Soft Tissue Sarcoma Ewing Sarcoma Collapse <<	Phase 1 Phase 2	Recruiting	June 30, 2021	Germany ... more >> Uniklinik RWTH Aachen Kinderklinik Recruiting Aachen, Germany Charite Virchow Kinderklinik - CC17 Recruiting Berlin, Germany Uniklinik Essen AoR Kinderklinik Recruiting Essen, Germany Klinik fur Kinder und Jugendmed - KKJM Recruiting Frankfurt, Germany Uniklinik Freiburg Kindermedizin Klinik IV Recruiting Freiburg, Germany Uniklinik Gottingen Kindermedizin Recruiting Gottingen, Germany Kinderklinik Muenchen Schwabing Not yet recruiting Muenchen, Germany Collapse <<
  NCT02015754	Colorectal Cancer	Phase 2	Completed	-	United States, Maryland ... more >> The Johns Hopkins Hospital Baltimore, Maryland, United States, 21287 Collapse <<

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