Topotecan Hydrochloride ( SKF104864) 是靶向拓扑异构酶I的细胞毒性剂,已进入临床试验。
Topotecan (synonym: NSC609699, Nogitecan HCl, SKFS 104864A) is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM, respectively.
Saline
0 μg/mL - 0.692 μg/mL
0.25 mg/mL腹腔注射给药
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Caceres G, et al. Anticancer Drugs. 2003, 14(7), 569-574.
[2] Uckun, F.M., et al. 1995. Blood. 85: 2817-2828.
[3] Arun, B., et al. 2001. Expert Opin Pharmacother. 2: 491-505.
分子式 C23H24ClN3O5 |
分子量 457.91 |
CAS号 119413-54-6 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 92 mg/mL |
Water 92 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01037023 | Lung Cancer, Small Cell | Drug: Topotecan | GlaxoSmithKline | 2010-10-01 | 2015-04-14 | |
NCT02303028 | Solid Tumors|Central Nervous System Tumors | Drug: Topotecan and Pazopanib | The Hospital for Sick Children|C17 Council | Phase 1|Phase 2 | 2015-03-01 | 2016-10-17 |
NCT01840943 | Epithelial Ovarian Cancer | Drug: CAELYX|Drug: Topotecan HCl | Xian-Janssen Pharmaceutical Ltd. | Phase 3 | 2013-06-01 | 2015-11-17 |
NCT02100007 | Solid Tumors | Drug: ME-344|Drug: Topotecan | MEI Pharma, Inc.|SCRI Development Innovations, LLC | Phase 1|Phase 2 | 2014-04-01 | 2016-07-01 |
NCT00002395 | HIV Infections|Leukoencephalopathy, Progressive Multifocal | Drug: Topotecan | SmithKline Beecham|NIH AIDS Clinical Trials Information Service | Phase 2 | null | 2005-06-23 |
NCT00611468 | Metastatic Solid Tumor | Drug: Topotecan|Drug: Erlotinib | Accelerated Community Oncology Research Network|GlaxoSmithKline|Genentech, Inc. | Phase 1 | 2006-06-01 | 2011-08-18 |
NCT02278510 | Malignant Glioma|WHO Grade III or IV Recurrent Glioma | Drug: Topotecan|Drug: Gadolinium DTPA|Device: Cleveland Multiport Catheter | Michael Vogelbaum, MD, PhD|Infuseon Therapeutics, Inc.|Case Comprehensive Cancer Center | Early Phase 1 | 2014-12-01 | 2016-09-19 |
NCT00294190 | Small Cell Lung Cancer|Carcinoma, Small Cell | Drug: Topotecan | SCRI Development Innovations, LLC|GlaxoSmithKline | Phase 2 | 2006-02-01 | 2012-12-06 |
NCT00382733 | Tumors | Drug: Oral Topotecan | Accelerated Community Oncology Research Network|GlaxoSmithKline | Phase 1|Phase 2 | 2006-11-01 | 2013-07-17 |
NCT01003938 | Ovarian Cancer | Drug: Topotecan|Drug: Erlotinib | New York University School of Medicine|OSI Pharmaceuticals | Phase 2 | 2009-08-01 | 2016-05-31 |
NCT00390806 | Lung Cancer, Non-Small Cell | Drug: HYCAMTIN, oral capsules|Radiation: Radiation | GlaxoSmithKline | Phase 3 | 2006-12-01 | 2013-12-05 |
NCT02500459 | Brain Tumor|High Grade Glioma | Drug: topotecan | Michael Vogelbaum, MD, PhD|Infuseon Therapeutics, Inc.|Case Comprehensive Cancer Center | Early Phase 1 | 2015-07-01 | 2016-01-26 |
NCT02963090 | Small Cell Lung Cancer | Drug: Topotecan|Drug: Pembrolizumab | Alliance Foundation Trials, LLC.|Merck Sharp & Dohme Corp. | Phase 2 | 2016-12-01 | 2016-11-10 |
NCT00158886 | Rectal Cancer | Drug: Hycamtin | GlaxoSmithKline | Phase 1 | 2001-11-01 | 2009-05-21 |
NCT02649673 | Small Cell Lung Cancer|Ovarian Cancer | Drug: LCL161|Drug: Topotecan | SCRI Development Innovations, LLC|Novartis Pharmaceuticals | Phase 1|Phase 2 | 2016-03-01 | 2016-09-26 |
NCT01600573 | Ovarian Cancer | Drug: pazopanib in combination with weekly topotecan | JSehouli|GlaxoSmithKline|Charite University, Berlin, Germany | Phase 1|Phase 2 | 2012-05-01 | 2016-10-10 |
NCT00610571 | Glioblastoma|Gliosarcoma|Anaplastic Astrocytoma | Drug: Oral Topotecan and Temodar | Katy Peters|GlaxoSmithKline|Schering-Plough|Duke University | Phase 1 | 2004-04-01 | 2013-10-23 |
NCT00483860 | Lung Cancer, Small Cell | Drug: Topotecan | GlaxoSmithKline | Phase 1 | 2007-06-01 | 2012-10-25 |
NCT00365547 | Lung Cancer | Biological: bevacizumab|Drug: topotecan hydrochloride | Masonic Cancer Center, University of Minnesota | Phase 2 | 2006-09-01 | 2012-07-31 |
NCT01736800 | Central Nervous System (CNS) Metastases|Brain Metastases | Drug: Topotecan|Drug: Temozolomide | The Methodist Hospital System | Phase 2 | 2007-03-01 | 2013-06-18 |
NCT00308165 | Brain Neoplasms, Primary Malignant | Procedure: Convection-Enhanced Delivery|Drug: Topotecan | Jeffrey N. Bruce|Columbia University | Phase 1|Phase 2 | 2004-03-01 | 2015-01-13 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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