Veliparib (ABT-888)是一种有效的PARP1和PARP2抑制剂,Ki分别为5.2 nM和2.9 nM,抑制SIRT2。
ABT-888, also named as Veliparib, is poly (ADP-ribose) polymerase (PARP) inhibitor and has demonstrated excellent in vivo efficacy in a broad spectrum of preclinical tumor models in combination with a variety of cytotoxic agents. PARP is involved in DNA repair and elevated PARP levels can result in resistance to cytotoxic chemotherapy and radiation. So, PARP inhibitors hold promise as chemotherapy and radiation sensitizers. ABT-888 is also active on microsatellite instability (MSI) cell lines harboring mutations in both MRE11 and RAD50 genes compared to microsatellite stable (MSS) cell lines (wild-type for both genes).
0.5% methylcellulose+0.2% Tween 80
10 μM
25或3.125 mg/kg 口服处理
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] Donawho CK, et al, Clin Cancer Res, 2007, 13 (9), 2728-2737.
分子式 C13H16N4O |
分子量 244.29 |
CAS号 912444-00-9 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 20 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02210663 | Advanced Solid Tumors | Drug: veliparib (ABT-888) | AbbVie | Phase 1 | 2014-07-01 | 2016-07-19 |
NCT02158507 | Metastatic Triple Negative Breast Cancer | Drug: Combination of Veliparib + Lapatinib | University of Alabama at Birmingham|Scariot Foundation|GlaxoSmithKline|AbbVie | 2014-07-01 | 2016-12-28 | |
NCT02289690 | Small Cell Lung Cancer | Drug: Veliparib|Drug: Carboplatin|Drug: Etoposide | AbbVie | Phase 2 | 2014-10-01 | 2017-02-22 |
NCT01853306 | Oncology|BRCA Mutated|High Grade Serous Ovarian Cancer|BRCA Mutated Breast Cancer | Drug: Veliparib | AbbVie | Phase 1 | 2013-03-01 | 2017-02-06 |
NCT01123876 | Gastric Cancer | Drug: Veliparib | AbbVie (prior sponsor, Abbott)|AbbVie | Phase 1 | 2010-03-01 | 2015-01-20 |
NCT01690598 | Ovarian Cancer | Drug: Veliparib|Drug: Topotecan | Vejle Hospital|Abbott | Phase 1|Phase 2 | 2012-11-01 | 2015-06-09 |
NCT01199224 | Solid Tumors | Drug: veliparib|Drug: veliparib|Drug: veliparib|Drug: veliparib | Abbott | Phase 1 | 2010-06-01 | 2011-02-03 |
NCT02723864 | Neoplasms | Drug: Veliparib + VX-970 + Cisplatin | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | Phase 1 | 2016-03-22 | 2017-03-21 |
NCT00892736 | Basal-Like Breast Carcinoma|BRCA1 Mutation Carrier|BRCA2 Mutation Carrier|Breast Carcinoma|Estrogen Receptor Negative|HER2/Neu Negative|Hereditary Breast and Ovarian Cancer Syndrome|Ovarian Carcinoma|Pancreatic Carcinoma|Progesterone Receptor Negative|Prostate Carcinoma|Recurrent Breast Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Solid Neoplasm|Triple-Negative Breast Carcinoma | Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Veliparib | National Cancer Institute (NCI) | Phase 1 | 2009-04-01 | 2016-06-30 |
NCT01351909 | HER2/Neu Negative|Recurrent Breast Carcinoma|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer | Drug: Cyclophosphamide|Other: Laboratory Biomarker Analysis|Drug: Veliparib | National Cancer Institute (NCI) | Phase 1 | 2011-05-01 | 2017-02-16 |
NCT01540565 | BRCA1 Mutation Carrier|BRCA2 Mutation Carrier|Ovarian Epithelial Tumor|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma | Other: Laboratory Biomarker Analysis|Drug: Veliparib | National Cancer Institute (NCI) | Phase 2 | 2012-04-01 | 2017-02-02 |
NCT01193140 | Solid Tumor Cancers | Drug: veliparib|Drug: Temozolomide | Abbott | Phase 2 | 2010-07-01 | 2012-11-16 |
NCT01434316 | BRCA1 Mutation Carrier|BRCA2 Mutation Carrier|Solid Neoplasm | Drug: Dinaciclib|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Veliparib | National Cancer Institute (NCI) | Phase 1 | 2011-11-01 | 2017-01-31 |
NCT01908478 | Pancreatic Cancer | Drug: Veliparib|Drug: Gemcitabine|Radiation: Intensity modulated radiation therapy | Cedars-Sinai Medical Center|AbbVie | Phase 1 | 2013-07-01 | 2017-02-17 |
NCT01589419 | Locally Advanced Rectal Cancer | Drug: veliparib|Drug: capecitabine|Radiation: radiation | AbbVie (prior sponsor, Abbott)|AbbVie | Phase 1 | 2012-06-01 | 2015-01-20 |
NCT02860819 | Testicular Cancer | Drug: Veliparib|Drug: Gemcitabine|Drug: Carboplatin | National Cancer Institute, Slovakia | Phase 2 | 2016-07-01 | 2016-08-04 |
NCT01472783 | Recurrent, Epithelial Ovarian Cancer | Drug: Veliparib | Vejle Hospital|Abbott | Phase 1|Phase 2 | 2011-11-01 | 2016-11-15 |
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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