Nelarabine是嘌呤核苷酸类似物,为DNA合成抑制剂,对肿瘤细胞的IC50为0.067-2.15 μM,可作用于T细胞急性淋巴细胞白血病。
Nelarabine is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.
0.125 μg/mL - 8 μg/mL
35 mg/kg静脉注射给药
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] Beesley AH, et al. Br J Haematol. 2007, 137(2), 109-116.
[2] DeAngelo DJ, et al. Nelarabine induces complete remissions in adults with relapsed or refractory T-lineage acute lymphoblastic leukemia or lymphoblastic lymphoma: Cancer and Leukemia Group B study 19801. Blood. 2007 Jun 15;109(12):5136-42.
分子式 C11H15N5O5 |
分子量 297.27 |
CAS号 121032-29-9 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 60 mg/mL |
Water 3 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01094860 | Leukemia | Drug: Nelarabine | M.D. Anderson Cancer Center|GlaxoSmithKline | Phase 1 | 2010-06-01 | 2016-12-16 |
NCT00866671 | Leukaemia, Lymphoblastic, Acute | Drug: nelarabine | GlaxoSmithKline | 2009-02-01 | 2015-01-12 | |
NCT01376115 | Cancer | Drug: Nelarabine | Novartis | 2008-01-01 | 2016-03-11 | |
NCT02763384 | T-Acute Lymphoblastic Leukemia|Adult T Lymphoblastic Lymphoma | Drug: BL-8040|Drug: Nelarabine | Washington University School of Medicine | Phase 2 | 2016-12-02 | 2017-02-02 |
NCT00005080 | Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Small Intestine Lymphoma|Stage I Cutaneous T-cell Non-Hodgkin Lymphoma|Stage I Mycosis Fungoides/Sezary Syndrome|Stage II Cutaneous T-cell Non-Hodgkin Lymphoma|Stage II Mycosis Fungoides/Sezary Syndrome|Stage III Cutaneous T-cell Non-Hodgkin Lymphoma|Stage III Mycosis Fungoides/Sezary Syndrome|Stage IV Cutaneous T-cell Non-Hodgkin Lymphoma|Stage IV Mycosis Fungoides/Sezary Syndrome | Drug: nelarabine | National Cancer Institute (NCI) | Phase 2 | 2000-05-01 | 2013-01-15 |
NCT00684619 | T-ALL, T-NHL (Lymphoblastic) | Drug: Nelarabine | Johann Wolfgang Goethe University Hospital | Phase 2 | 2003-06-01 | 2010-08-20 |
NCT00981799 | Relapsed T-Cell Acute Lymphoblastic Leukemia|Relapsed T-Cell Lymphoblastic Lymphoma | Drug: Nelarabine|Drug: Etoposide|Drug: Cyclophosphamide|Drug: Methotrexate|Drug: Filgrastim | Therapeutic Advances in Childhood Leukemia Consortium|GlaxoSmithKline|Novartis | Phase 1|Phase 2 | 2010-06-01 | 2015-11-20 |
NCT00501826 | Leukemia|Lymphoblastic Lymphoma|Leukemia, Lymphoblastic, Acute | Drug: Doxorubicin|Drug: Cyclophosphamide|Drug: Cytarabine|Drug: Dexamethasone|Drug: Methotrexate|Drug: Vincristine|Drug: Nelarabine | M.D. Anderson Cancer Center|Novartis | Phase 2 | 2007-07-01 | 2017-03-23 |
NCT00005982 | Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome | Drug: nelarabine|Other: pharmacological study | National Cancer Institute (NCI) | Phase 2 | 2000-04-01 | 2013-01-22 |
NCT00005950 | Angioimmunoblastic T-cell Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Small Lymphocytic Lymphoma|Splenic Marginal Zone Lymphoma|Waldenstr枚m Macroglobulinemia | Drug: nelarabine | National Cancer Institute (NCI) | Phase 2 | 2000-04-01 | 2013-01-22 |
NCT00406757 | Leukaemia, Lymphoblastic, Acute and Lymphoma, Lymphoblastic|Lymphoblastic Lymphoma|Acute Lymphoblastic Leukemia | Drug: Nelarabine injection 400mg/m2|Drug: Nelarabine injection 650mg/m2|Drug: Nelarabine injection 1000mg/m2|Drug: Nelarabine injection 1500mg/m2 | GlaxoSmithKline | Phase 1 | 2006-08-01 | 2012-05-31 |
NCT02619630 | T-cell Adult Acute Lymphoblastic Leukemia | Drug: nelarabine | Assistance Publique - H么pitaux de Paris | Phase 2 | 2015-12-01 | 2016-06-23 |
NCT00003545 | Leukemia|Lymphoma | Drug: nelarabine | National Cancer Institute (NCI)|Southwest Oncology Group | Phase 2 | 1998-08-01 | 2013-02-04 |
NCT00004239 | Chronic Myeloproliferative Disorders|Leukemia|Lymphoma|Multiple Myeloma and Plasma Cell Neoplasm|Myelodysplastic Syndromes | Drug: Compound 506U78 | Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) | Phase 1 | 1999-12-01 | 2016-07-01 |
NCT00003837 | Leukemia|Lymphoma | Drug: nelarabine | National Cancer Institute (NCI) | 1999-09-01 | 2013-06-18 | |
NCT00006020 | Leukemia | Drug: nelarabine | Southwest Oncology Group|National Cancer Institute (NCI) | Phase 2 | 2000-07-01 | 2015-03-05 |
NCT00003635 | Leukemia | Drug: nelarabine | GlaxoSmithKline|National Cancer Institute (NCI) | Phase 2 | 1999-01-01 | 2013-07-17 |
NCT00002970 | Recurrent Childhood Acute Lymphoblastic Leukemia|Recurrent Childhood Lymphoblastic Lymphoma|T-cell Childhood Acute Lymphoblastic Leukemia | Drug: nelarabine|Drug: methotrexate|Drug: cytarabine|Drug: therapeutic hydrocortisone | National Cancer Institute (NCI)|Children's Cancer Group | Phase 2 | 1997-06-01 | 2013-07-01 |
NCT02881086 | Acute Lymphoblastic Leukemia|Lymphoblastic Lymphoma | Drug: Rituximab|Drug: Nelarabine|Drug: PEG-Asparaginase|Procedure: Cranial irradiation|Drug: Imatinib|Drug: Idarubicin|Drug: Dexamethasone|Drug: Cyclophosphamide|Drug: Fludarabine|Drug: Vincristine|Drug: Mercaptopurine|Drug: VP16|Drug: Daunorubicin (DNR)|Drug: Methotrexate|Procedure: Stem cell transplantation|Drug: Cytarabine|Drug: Vindesine|Drug: Adriamycin|Drug: Prednisolone | Johann Wolfgang Goethe University Hospital | Phase 3 | 2016-08-01 | 2016-08-23 |
NCT01085617 | Leukemia|Mucositis|Oral Complications | Biological: palifermin|Biological: rituximab|Drug: cyclophosphamide|Drug: cytarabine|Drug: daunorubicin hydrochloride|Drug: etoposide|Drug: fludarabine phosphate|Drug: imatinib mesylate|Drug: melphalan|Drug: mercaptopurine|Drug: methotrexate|Drug: nelarabine|Drug: pegaspargase|Drug: vincristine sulfate|Procedure: allogeneic hematopoietic stem cell transplantation|Procedure: assessment of therapy complications|Radiation: total-body irradiation | University College London Hospitals|National Cancer Institute (NCI) | Phase 3 | 2010-01-01 | 2013-08-23 |
NCT00408005 | Adult T Acute Lymphoblastic Leukemia|Childhood T Acute Lymphoblastic Leukemia|Stage II Adult T-Cell Leukemia/Lymphoma|Stage II Childhood Lymphoblastic Lymphoma|Stage II Contiguous Adult Lymphoblastic Lymphoma|Stage II Non-Contiguous Adult Lymphoblastic Lymphoma|Stage III Adult Lymphoblastic Lymphoma|Stage III Adult T-Cell Leukemia/Lymphoma|Stage III Childhood Lymphoblastic Lymphoma|Stage IV Adult Lymphoblastic Lymphoma|Stage IV Adult T-Cell Leukemia/Lymphoma|Stage IV Childhood Lymphoblastic Lymphoma|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Childhood Acute Lymphoblastic Leukemia | Drug: Asparaginase|Drug: Cyclophosphamide|Drug: Cytarabine|Drug: Daunorubicin Hydrochloride|Drug: Dexamethasone|Drug: Doxorubicin Hydrochloride|Other: Laboratory Biomarker Analysis|Drug: Leucovorin Calcium|Drug: Mercaptopurine|Drug: Methotrexate|Drug: Nelarabine|Drug: Pegaspargase|Drug: Prednisone|Radiation: Radiation Therapy|Drug: Thioguanine|Drug: Vincristine Sulfate | National Cancer Institute (NCI) | Phase 3 | 2007-01-01 | 2017-03-14 |
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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