BMN 673是一种新型的PARP抑制剂,IC50为0.58 nM,也有效抑制PARP-2,但不抑制PARG,对PTEN突变型高度敏感。
Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.58 nM in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.
0.33 mg/kg/day,每天一次口服处理
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] Wang B, et al. Molecular Cancer Therapeutics, 2009, 8 (12 Suppl), A121.
分子式 C19H14F2N6O |
分子量 380.35 |
CAS号 1207456-01-6 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 35 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT02282345 | Breast Cancer | Drug: Talazoparib | M.D. Anderson Cancer Center|Medivation, Inc. | Phase 2 | 2015-04-01 | 2017-03-16 |
NCT03070548 | Advanced Solid Tumors | Drug: Talazoparib | Medivation, Inc. | Phase 1 | 2016-10-01 | 2017-02-28 |
NCT01286987 | Advanced or Recurrent Solid Tumors|Breast Neoplasms|Ovarian Cancer, Epithelial|Ewing Sarcoma|Small Cell Lung Carcinoma|Prostate Cancer|Pancreas Cancer | Drug: Talazoparib | Medivation, Inc. | Phase 1 | 2010-12-01 | 2016-03-09 |
NCT03042910 | Solid Tumor | Drug: Talazoparib | Medivation, Inc. | Phase 1 | 2016-10-01 | 2017-02-01 |
NCT02567396 | Estrogen Receptor Negative|Head and Neck Squamous Cell Carcinoma|HER2/Neu Negative|Hormone-Resistant Prostate Cancer|Metastatic Pancreatic Adenocarcinoma|Progesterone Receptor Negative|Solid Neoplasm|Stage III Mesothelioma|Stage IIIA Gastric Cancer|Stage IIIA Non-Small Cell Lung Cancer|Stage IIIA Ovarian Cancer|Stage IIIA Small Cell Lung Carcinoma|Stage IIIB Gastric Cancer|Stage IIIB Non-Small Cell Lung Cancer|Stage IIIB Ovarian Cancer|Stage IIIB Small Cell Lung Carcinoma|Stage IIIC Gastric Cancer|Stage IIIC Ovarian Cancer|Stage IV Mesothelioma|Stage IV Non-Small Cell Lung Cancer|Stage IV Ovarian Cancer|Stage IV Small Cell Lung Carcinoma|Triple-Negative Breast Carcinoma | Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Talazoparib | National Cancer Institute (NCI) | Phase 1 | 2016-07-01 | 2017-02-06 |
NCT02997163 | Advanced Solid Tumors | Drug: Talazoparib | Medivation, Inc. | Phase 1 | 2017-01-01 | 2016-12-15 |
NCT02997176 | Advanced Solid Tumors | Drug: Talazoparib | Medivation, Inc. | Phase 1 | 2016-11-01 | 2016-12-15 |
NCT02286687 | Advanced Cancers | Drug: Talazoparib Tosylate|Behavioral: Phone Call | M.D. Anderson Cancer Center|BioMarin Pharmaceutical | Phase 2 | 2014-12-22 | 2017-02-06 |
NCT02401347 | Advanced Breast Cancer|HER2/Neu Negative|Triple-Negative Breast Cancer | Drug: Talazoparib Tosylate | Melinda Telli|National Cancer Institute (NCI)|Stanford University | Phase 2 | 2015-08-01 | 2015-08-09 |
NCT02034916 | Breast Neoplasms|BRCA 1 Gene Mutation|BRCA 2 Gene Mutation | Drug: talazoparib | Medivation, Inc.|Myriad Genetic Laboratories, Inc. | Phase 2 | 2014-01-01 | 2016-12-13 |
NCT02836028 | Ovarian Cancer | Drug: Talazoparib|Drug: Temozolomide | Medivation, Inc.|Myriad Genetic Laboratories, Inc. | Phase 2 | 2016-10-01 | 2016-12-20 |
NCT02878785 | Acute Myeloid Leukemia | Drug: Decitabine|Drug: talazoparib | University of Maryland|Medivation, Inc. | Phase 1|Phase 2 | 2016-08-01 | 2016-08-21 |
NCT02627430 | Adult Solid Neoplasm|Estrogen Receptor Negative|Fallopian Tube Serous Neoplasm|HER2/Neu Negative|Ovarian Serous Adenocarcinoma|Ovarian Serous Tumor|Primary Peritoneal Serous Adenocarcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Triple-Negative Breast Carcinoma | Drug: Hsp90 Inhibitor AT13387|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Talazoparib | National Cancer Institute (NCI) | Phase 1 | 2016-03-01 | 2016-07-22 |
NCT02392793 | Childhood Solid Tumors | Drug: Talazoparib|Drug: Irinotecan|Drug: Temozolomide|Drug: Filgrastim|Drug: Peg-filgrastim | St. Jude Children's Research Hospital|BioMarin Pharmaceutical|Alliance Pharma|Pfizer | Phase 1 | 2015-03-16 | 2017-02-08 |
NCT02921919 | Cancer | Drug: Talazoparib | Medivation, Inc. | Phase 2 | 2016-09-01 | 2017-01-31 |
NCT02317874 | Solid Neoplasm | Drug: Carboplatin|Other: Laboratory Biomarker Analysis|Drug: Paclitaxel|Other: Pharmacological Study|Drug: Talazoparib | National Cancer Institute (NCI) | Phase 1 | 2015-07-01 | 2017-03-22 |
NCT01945775 | Breast Neoplasms|BRCA 1 Gene Mutation|BRCA 2 Gene Mutation | Drug: talazoparib|Drug: Physician's-Choice | Medivation, Inc. | Phase 3 | 2013-10-01 | 2016-12-08 |
NCT02537561 | Solid Tumors|Carcinoma, Non-Small Cell Lung|Non-Small Cell Lung Cancer|Non-Small-Cell Lung Carcinoma|Nonsmall Cell Lung Cancer | Drug: Cisplatin|Drug: Gemcitabine|Drug: Talazoparib | Washington University School of Medicine|BioMarin Pharmaceutical | Phase 1 | 2015-12-01 | 2016-02-10 |
NCT02116777 | Adult Solid Neoplasm|Childhood Solid Neoplasm|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Childhood Acute Lymphoblastic Leukemia|Recurrent Childhood Central Nervous System Neoplasm|Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor|Refractory Central Nervous System Neoplasm | Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Talazoparib|Drug: Temozolomide | National Cancer Institute (NCI) | Phase 1|Phase 2 | 2014-05-01 | 2017-03-22 |
NCT02316834 | Fallopian Tube Cancer|Ovarian Cancer|Peritoneal Cancer | Drug: BMN 673 | M.D. Anderson Cancer Center|BioMarin Pharmaceutical|National Cancer Institute (NCI) | Early Phase 1 | 2015-06-01 | 2017-02-24 |
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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