Carboplatin (卡铂) 能与DNA结合,干扰细胞修复。
Carboplatin is a second generation potent platinum-based antineoplastic agent that is believed to form inter- and intrastrand DNA adducts which activate signaling pathways culminating in apoptosis. Carboplatin is a DNA synthesis inhibitor by binding to DNA and interfering with the cell's repair mechanism. Antitumor agent that forms platinum-DNA adducts. Causes intra- and interstrand DNA crosslinks blocking DNA replication and transcription. The development of carboplatin was inspired from the efficacy of its progenitor, Carboplatin displays potent antitumor activity and lower nephrotoxicity than Cisplatin. The action of this group of platinum-based compounds is primarily attributed to DNA adduct formation, however, these molecules also bind other biological molecules, including enzymes, which might play a role in their mechanism of action.
30% PEG 400+0.5% Tween 80+5% Propylene glycol+ddH2O
0 - 200 μM
≤60 mg/kg 腹腔注射
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] Banerji U, et al. Cancer Chemother Pharmacol. 2008, 62(5), 769-778.
[2] Harland, S.J., et al. 1984. Cancer Res. 44: 1693-1697.
[3] Smith, I.E., et al. 1985. Cancer Treat Rep. 69: 43-46.
[4] Smith, I.E. and Evans, B.D. 1985. Cancer Treat. Rev. 12: 73-75.
[5] Lokich, J. 2001. Cancer Invest. 19: 756-760.
分子式 C6H12N2O4Pt |
分子量 371.25 |
CAS号 41575-94-4 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO <1 mg/mL |
Water >10 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02137928 | Retinoblastoma | Drug: carboplatin periocular injection|Drug: chemotherapy | Sun Yat-sen University | Phase 3 | 2006-01-01 | 2014-12-18 |
NCT01261299 | Carcinoma, Non-Small-Cell Lung|Urinary Bladder Neoplasms | Drug: Carbon-14-labeled carboplatin | University of California, Davis|Lawrence Livermore National Laboratory|National Institutes of Health (NIH) | Early Phase 1 | 2010-12-01 | 2017-03-21 |
NCT00230542 | Ovarian Cancer|Peritoneal Cancer|Fallopian Tube Cancer | Drug: Carboplatin|Drug: Pemetrexed | Dana-Farber Cancer Institute|Massachusetts General Hospital|Brigham and Women's Hospital | Phase 2 | 2005-09-01 | 2017-03-22 |
NCT02279992 | Glioma|Brain Neoplasms|Brain Metastasis | Drug: Vardenafil|Drug: Carboplatin | Cedars-Sinai Medical Center | Early Phase 1 | 2011-05-01 | 2015-10-21 |
NCT02103244 | Cancer | Drug: Carboplatin | Rijnstate Hospital | Phase 4 | 2014-09-01 | 2014-04-02 |
NCT00889018 | Intraocular Retinoblastoma | Drug: carboplatin|Drug: carboplatin | All India Institute of Medical Sciences, New Delhi|Council of Scientific and Industrial Research, India | 2009-04-01 | 2012-02-07 | |
NCT01051362 | Non-small Cell Lung Cancer | Drug: PLD and Carboplatin | The First Affiliated Hospital of Guangzhou Medical University | Phase 2 | 2006-02-01 | 2010-01-15 |
NCT02199171 | FIGO Stage IIC-IV Ovarian Carcinoma|Fallopian Tube Carcinoma|Peritoneal Carcinoma | Drug: carboplatin | University of California, Irvine | Phase 1 | 2014-07-01 | 2014-09-17 |
NCT02035345 | Recurrent Ovarian Cancer|Platinum Sensitive Ovarian Cancer | Drug: Carboplatin | Massachusetts General Hospital | Phase 4 | 2014-01-01 | 2016-11-01 |
NCT02339753 | Pediatric Solid Tumor | Drug: Carboplatin | The Korean Society of Pediatric Hematology Oncology | Phase 2 | 2015-01-01 | 2015-01-15 |
NCT00675545 | Hormone-Refractory Prostate Cancer | Drug: Docetaxel, Carboplatin | National University Hospital, Singapore | Phase 2 | 2007-05-01 | 2012-03-30 |
NCT01542047 | Cancer, Metastatic | Drug: Carboplatin|Drug: Pazopanib | New Mexico Cancer Care Alliance|GlaxoSmithKline | Phase 1 | 2012-08-01 | 2015-06-17 |
NCT02734069 | Lung Cancer|Sarcopenia|Toxicity | Drug: Carboplatin | Instituto Nacional de Cancerologia de Mexico | 2016-02-01 | 2016-04-11 | |
NCT01178112 | Advanced Cancers | Drug: Trientine|Drug: Carboplatin|Drug: Trientine MTD|Drug: Carboplatin MTD|Other: PK Testing | M.D. Anderson Cancer Center | Phase 1 | 2010-07-01 | 2015-11-16 |
NCT00702962 | Small Cell Lung Cancer | Drug: Vorinostat, Carboplatin, Etoposide|Other: SAHA | Milton S. Hershey Medical Center|Merck Sharp & Dohme Corp. | Phase 1|Phase 2 | 2008-09-01 | 2017-01-26 |
NCT02133625 | Advanced Solid Tumor|Metastatic Solid Tumor | Drug: carboplatin|Drug: pioglitazone | Dana-Farber Cancer Institute | Phase 1 | 2011-08-01 | 2016-05-12 |
NCT02684227 | Endometrial Cancer | Drug: Enzalutamide|Drug: Carboplatin|Drug: Paclitaxel | M.D. Anderson Cancer Center|Astellas Pharma Inc|Medivation, Inc.|National Comprehensive Cancer Network | Phase 2 | 2016-08-01 | 2016-12-01 |
NCT01644955 | Adult Anaplastic Astrocytoma|Adult Anaplastic Oligodendroglioma|Recurrent Adult Brain Tumor | Drug: carboplatin|Procedure: Surgery | James Elder|Ohio State University Comprehensive Cancer Center | Phase 1 | 2012-06-01 | 2016-07-19 |
NCT02941523 | Cancer | Drug: NOX66|Drug: Carboplatin | Noxopharm Limited | Phase 1|Phase 2 | 2017-03-03 | 2017-03-04 |
NCT00362817 | Brain Tumor|Brain Metastases | Drug: carboplatin|Drug: temozolomide | Ohio State University Comprehensive Cancer Center | Phase 1|Phase 2 | 2004-10-01 | 2015-05-04 |
NCT00735878 | Non Small Cell Lung Cancer|Advanced Lung Cancer | Drug: ABT-751 and Carboplatin | Dartmouth-Hitchcock Medical Center|Abbott | Phase 1|Phase 2 | 2004-09-01 | 2009-04-29 |
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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