Mitoxantrone HCl是II型拓扑异构酶抑制剂,有抗肿瘤活性。
Mitoxantrone dihydrochloride is a potent inhibitor of topoisomerase II. Induces DNA damage by intercalating into DNA and inhibiting Topo II (topoisomerase II). Mitoxantrone dihydrochloride induces interstrand DNA cross-links and DNA-protein cross-links in cellular systems. Mitoxantrone dihydrochloride has recently been shown to be an inhibitor of DNA methylation.
Saline
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] Seitz M. Curr Opin Rheumatol, 1999, 11(3), 226-232.
[2] Mitoxantrone and ametantrone induce interstrand cross-links in DNA of tumour cells: A. Skladanowski & J. Konopa; Br. J. Cancer 82, 1300 (2000)
[3] A molecular understanding of mitoxantrone-DNA adduct formation: effect of cytosine methylation and flanking sequences: B.S. Parker, et al.; J. Biol. Chem. 279, 18814 (2004)
分子式 C22H30Cl2N4O6 |
分子量 517.4 |
CAS号 70476-82-3 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 88 mg/mL |
Water 88 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02043756 | Neoplasms | Drug: Mitoxantrone Hydrochloride Liposome|Drug: Mitoxantrone | CSPC ZhongQi Pharmaceutical Technology Co., Ltd. | Phase 1 | 2011-08-01 | 2014-01-21 |
NCT02597387 | Relapsed DLBCL and PT/NKCLs | Drug: Mitoxantrone HCL Liposome Injection | CSPC ZhongQi Pharmaceutical Technology Co., Ltd. | Phase 2 | 2015-08-01 | 2015-11-04 |
NCT00203073 | Relapsing Remitting Multiple Sclerosis | Drug: glatiramer acetate 20 mg|Drug: glatiramer acetate 20 mg, with mitoxantrone | Teva Pharmaceutical Industries | Phase 2 | 2003-06-01 | 2011-04-13 |
NCT00882076 | Leukemia | Drug: Etoposide, Mitoxantrone, Clofarabine|Drug: Clofarabine, Etoposide, Mitoxantrone | Milton S. Hershey Medical Center | Phase 1 | 2009-03-01 | 2014-12-04 |
NCT01842672 | Acute Lymphoblastic Leukemia|Acute Myelogenous Leukemia|Lymphoblastic Lymphoma|Diffuse Large B-cell Lymphoma|Burkitt Lymphoma/Leukemia | Drug: Clofarabine|Drug: Mitoxantrone | New York Medical College | Phase 1|Phase 2 | 2013-03-01 | 2016-07-29 |
NCT00660036 | Acute Myeloid Leukemia | Drug: Gemtuzumab ozogamicin|Drug: Mitoxantrone|Drug: Etoposide | University of Pittsburgh | Phase 1 | 2008-09-01 | 2016-01-14 |
NCT00268242 | Leukemia | Drug: Gemcitabine Hydrochloride|Drug: Mitoxantrone Hydrochloride | The Cleveland Clinic|National Cancer Institute (NCI)|Duke University | Phase 2 | 2006-01-01 | 2015-08-30 |
NCT00059631 | Prostate Cancer | Drug: Mitoxantrone (Novantrone)|Drug: Bortezomib (PS-341) | M.D. Anderson Cancer Center|Millennium Pharmaceuticals, Inc.|National Cancer Institute (NCI) | Phase 1 | 2003-03-01 | 2015-06-19 |
NCT01627938 | Multiple Sclerosis | Drug: Dexrazoxane (DRZ) plus Mitoxantrone (MX)|Drug: Placebo plus Mitoxantrone (MX) | PD Dr. Andrew Chan|Ruhr University of Bochum | Phase 2 | 2012-04-01 | 2014-11-04 |
NCT02021825 | Neuromyelitis Optica|Neuromyelitis Optica Spectrum Disorders | Drug: Mitoxantrone | Xuanwu Hospital, Beijing | Phase 4 | 2009-03-01 | 2013-12-19 |
NCT01594918 | Metastatic Castration-resistant Prostate Cancer | Drug: Cabazitaxel|Drug: Mitoxantrone|Drug: Prednisone|Drug: Pegfilgrastim | Rahul Aggarwal|Sanofi|University of California, San Francisco | Phase 1 | 2012-06-01 | 2016-10-24 |
NCT02131688 | Malignant Lymphoma | Drug: Mitoxantrone Hydrochloride Liposome | CSPC ZhongQi Pharmaceutical Technology Co., Ltd. | Phase 1 | 2013-05-01 | 2014-05-04 |
NCT00661492 | Androgen-independent Prostate Cancer | Drug: cetuximab|Drug: Mitoxantrone | US Oncology Research|ImClone LLC|Oregon Health and Science University | Phase 2 | 2008-05-01 | 2016-10-13 |
NCT00940524 | Leukemia|Acute Lymphoblastic Leukemia | Drug: Dasatinib, Mitoxantrone, Cytarabine | Memorial Sloan Kettering Cancer Center|Bristol-Myers Squibb | Phase 1 | 2009-07-01 | 2014-04-09 |
NCT00447473 | Prostatic Neoplasms | Drug: GM-CSF|Drug: Ketoconazole|Drug: Mitoxantrone | The Methodist Hospital System|Bayer | Phase 2 | 2006-07-01 | 2016-03-15 |
NCT01214317 | Multiple Sclerosis | Procedure: plasmapheresis | Isfahan University of Medical Sciences | 2010-01-01 | 2011-08-16 | |
NCT00901927 | Follicular Lymphoma | Drug: Bendamustine|Drug: Mitoxantrone|Drug: Rituximab | M.D. Anderson Cancer Center|Cephalon | Phase 2 | 2009-05-01 | 2016-05-26 |
NCT02597153 | Relapsed Cutaneous T Cell Lymphom | Drug: Mitoxantrone HCL Liposome Injection | CSPC ZhongQi Pharmaceutical Technology Co., Ltd. | Phase 2 | 2015-10-01 | 2015-11-03 |
NCT00003858 | Prostate Cancer | Drug: mitoxantrone hydrochloride | Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) | Phase 2 | null | 2016-07-12 |
NCT01839240 | Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia in Remission|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Del(5q)|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Recurrent Adult Acute Myeloid Leukemia|Secondary Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia | Drug: azacitidine|Drug: cytarabine|Drug: mitoxantrone hydrochloride|Other: laboratory biomarker analysis | University of Chicago|National Cancer Institute (NCI) | Phase 1 | 2012-06-01 | 2016-10-24 |
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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