Voreloxin能抑制拓扑异构酶II,有抗肿瘤活性。
Voreloxin is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.
~10 微克/毫升
~50 mg/kg 腹腔注射
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] Tsuzuki Y, et al. J Med Chem. 2004, 47(8), 2097-2109.
[2] Advani, Ranjana H.; Hurwitz, Herbert I.; Gordon, Michael S. et al. Voreloxin, a First-in-Class Anticancer Quinolone Derivative, in Relapsed/Refractory Solid Tumors: A Report on Two Dosing Schedules. Clinical Cancer Research (2010), 16(7), 2167-2175.
[3] Scatena, Caroline D.; Kumer, Jeffrey L.; Arbitrario, Jennifer P. et al. Voreloxin, a first-in-class anticancer quinolone derivative, acts synergistically with cytarabine in vitro and induces bone marrow aplasia in vivo. Cancer Chemotherapy and Pharmacology (2010), 66(5), 881-888.
[4] Abbas JA, Stuart RK. Vosaroxin : a novel antineoplastic quinolone. Expert Opin Investig Drugs. 2012 Aug;21(8):1223-33.
分子式 C18H19N5O4S |
分子量 401.44 |
CAS号 175414-77-4 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 10 mM |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT00541866 | Acute Myeloid Leukemia | Drug: voreloxin injection and cytarabine | Sunesis Pharmaceuticals | Phase 1|Phase 2 | 2007-08-01 | 2012-06-05 |
NCT00607997 | Leukemia|Acute Disease|Acute Myeloid Leukemia|Nonlymphocytic Leukemia|Myelodysplastic Syndromes | Drug: voreloxin | Sunesis Pharmaceuticals | Phase 2 | 2008-04-01 | 2012-06-05 |
NCT00408603 | Epithelial Ovarian Cancer | Drug: Voreloxin Injection | Sunesis Pharmaceuticals | Phase 2 | 2006-11-01 | 2012-06-05 |
NCT01913951 | Myelodysplastic Syndromes | Drug: vosaroxin|Drug: Azacitidine | Washington University School of Medicine | Phase 1 | 2013-11-22 | 2017-02-18 |
NCT01980056 | Myelodysplastic Syndrome | Drug: Vosaroxin | Weill Medical College of Cornell University|Sunesis Pharmaceuticals | Phase 1|Phase 2 | 2013-10-25 | 2017-03-01 |
NCT00246662 | Leukemia, Lymphocytic, Acute|Leukemia, Nonlymphocytic, Acute|Leukemia, Myeloid, Chronic|Myelodysplastic Syndromes | Drug: Vosaroxin | Sunesis Pharmaceuticals | Phase 1 | 2005-11-01 | 2017-02-06 |
NCT02658487 | Acute Myeloid Leukemia|Acute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome|Acute Myeloid Leukemia With Multilineage Dysplasia|Myeloid Sarcoma|Secondary Acute Myeloid Leukemia|Therapy-Related Acute Myeloid Leukemia|Therapy-Related Myelodysplastic Syndrome | Drug: Cytarabine|Drug: Vosaroxin | Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) | Phase 2 | 2016-03-01 | 2016-10-06 |
NCT01893320 | Leukemia | Drug: Vosaroxin|Drug: Decitabine | M.D. Anderson Cancer Center|Sunesis Pharmaceuticals | Phase 1|Phase 2 | 2013-07-18 | 2017-02-03 |
NCT01191801 | Leukemia|Acute Myeloid Leukemia|Acute Nonlymphocytic Leukemia | Drug: vosaroxin and cytarabine|Drug: placebo and cytarabine | Sunesis Pharmaceuticals | Phase 3 | 2010-10-01 | 2013-10-10 |
NCT02485353 | Leukemia, Myeloid, Acute | Drug: Vosaroxin and Cytarabine | Hamid Sayar|Indiana University | 2015-10-01 | 2016-08-24 | |
NCT00091585 | Neoplasms | Drug: SNS-595 | Sunesis Pharmaceuticals | Phase 1 | 2004-06-01 | 2007-05-09 |
NCT00094159 | Neoplasms | Drug: SNS-595 | Sunesis Pharmaceuticals | Phase 1 | 2004-10-01 | 2007-05-09 |
NCT00298896 | Carcinoma, Small Cell|Small Cell Lung Cancer | Drug: SNS-595 Injection | Sunesis Pharmaceuticals | Phase 2 | 2006-02-01 | 2009-03-05 |
NCT00252382 | Carcinoma, Non-Small-Cell Lung | Drug: SNS-595 Injection | Sunesis Pharmaceuticals | Phase 2 | 2005-11-01 | 2007-05-09 |
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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