Tasquinimod(ABR-215050)是喹啉-3-甲酰胺利诺胺类似物,具有抗血管生成和抗肿瘤活性。
Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.
~30 mg/kg/dp.o.
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] Isaacs JT, et al. Cancer Res.?013, 73(4), 1386-1399.
分子式 C20H17F3N2O4 |
分子量 406.36 |
CAS号 254964-60-8 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 80 mg/mL |
Water <1 mg/mL |
Ethanol 10 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01234311 | Prostate Cancer | Drug: tasquinimod|Drug: Placebo | Active Biotech AB | Phase 3 | 2011-03-01 | 2015-10-02 |
NCT02396368 | Prostate Cancer|Bone-only Metastatic Castration-Resistant Prostate Cancer (CRPC) | Drug: Tasquinimod|Radiation: Radium 223 | Sidney Kimmel Comprehensive Cancer Center | Phase 1 | 2015-03-01 | 2015-11-17 |
NCT01048203 | Healthy | Drug: ABR-215050 | Active Biotech AB | Phase 1 | 2009-01-01 | 2014-08-26 |
NCT01513733 | Prostate Cancer | Drug: tasquinimod|Drug: tasquinimod 0.25 mg; 0.5 mg|Drug: tasquinimod 0.25 mg; 0.5 mg; 1.0 mg | Andrew J. Armstrong, MD|Duke University | Phase 1 | 2012-01-01 | 2017-02-08 |
NCT02159950 | Hormone-Resistant Prostate Cancer|Metastatic Prostate Carcinoma|Recurrent Prostate Carcinoma|Stage IV Prostate Cancer | Other: Laboratory Biomarker Analysis|Biological: Sipuleucel-T|Drug: Tasquinimod | Roswell Park Cancer Institute|National Cancer Institute (NCI)|Active Biotech AB | Phase 2 | 2015-01-01 | 2016-05-19 |
NCT01743469 | Advanced or Metastatic Hepatocellular Cancer|Advanced or Metastatic Ovarian Cancer|Metastatic Renal Cell Cancer|Advanced or Metastatic Gastric Carcinoma | Drug: Tasquinimod | Ipsen | Phase 2 | 2012-12-01 | 2016-03-31 |
NCT01732549 | Metastatic Castrate Resistant Prostate Cancer | Drug: Tasquinimod|Drug: Placebo | Ipsen | Phase 2 | 2013-01-01 | 2016-08-09 |
NCT02057666 | Asian Chemo-nave Patients With Metastatic Castrate-resistant Prostate Cancer | Drug: Tasquinimod|Drug: Placebo | Ipsen | Phase 3 | 2014-01-01 | 2015-06-29 |
NCT00560482 | Prostate Cancer | Drug: ABR-215050, tasquinimod|Drug: Placebo | Active Biotech AB | Phase 2 | 2007-12-01 | 2015-10-02 |
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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