Floxuridine (氟脲苷; 5-fluorodeoxyuridine)为抗代谢剂,可抑制PEPT1,GI50为5.1 μM。
Floxuridine is an antineoplastic antimetabolite, used in the treatment of colon carcinoma and colorectal cancer that has metastasized to the liver.
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] Tsume Y, et al. Mol Pharm, 2008, 5(5), 717-727.
[2] Huehls et al (2012) Poly(ADP-ribose) polymerase inhibition synergizes with 5-fluorodeoxyuridine but not 5-fluorouracil in ovarian cancer cells. Cancer Res. 71 4944.
[3] Bapat et al (1983) Human leukemic cells resistant to 5-fluoro-2'-deoxyuridine contain a thymidylate synthetase with lower affinity for nucleotides. J.Biol.Chem. 258 4130.
[4] Wyatt and Wilson (2009) Participation of DNA repair in the response to 5-fluorouracil. Cell.Mol.Life Sci. 66 788.
分子式 C9H11FN2O5 |
分子量 246.19 |
CAS号 50-91-9 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 48 mg/mL |
Water 50 mg/mL |
Ethanol 10 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01749397 | Stage IV Fallopian Tube Cancer|Stage IV Ovarian Cancer|Stage IV Primary Peritoneal Cancer | Drug: Floxuridine|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Veliparib | National Cancer Institute (NCI) | Phase 1 | 2012-12-01 | 2017-01-31 |
NCT00695201 | Colon Cancer|Rectal Cancer | Drug: Floxuridine, Oxaliplatin, CPT-11|Drug: Floxuridine, Oxaliplatin, CPT-11 | Memorial Sloan Kettering Cancer Center|University of Medicine and Dentistry of New Jersey|Rutgers, The State University of New Jersey|Sanofi | Phase 1 | 2000-08-01 | 2016-09-22 |
NCT00268463 | Colorectal Cancer|Metastatic Cancer | Drug: capecitabine|Drug: floxuridine|Drug: oxaliplatin | NSABP Foundation Inc|National Cancer Institute (NCI) | Phase 3 | 2006-01-01 | 2013-05-10 |
NCT00848783 | Gastric Cancer|Gastric Adenocarcinoma|Esophageal Cancer | Drug: Irinotecan|Drug: Cisplatin|Procedure: Surgery|Drug: Floxuridine|Drug: Capecitabine | New York University School of Medicine | Phase 2 | 2008-05-01 | 2016-06-17 |
NCT00063960 | Colorectal Cancer|Metastatic Cancer | Drug: floxuridine|Drug: irinotecan hydrochloride | Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) | Phase 2 | 2003-08-01 | 2016-07-01 |
NCT00361842 | Colorectal Neoplasms | Drug: CPX-1 (Irinotecan HCl:Floxuridine) Liposome Injection | Celator Pharmaceuticals | Phase 2 | 2006-07-01 | 2016-07-25 |
NCT00001576 | Colorectal Neoplasm|Liver Neoplasm|Neoplasm Metastasis | Drug: Melphalan|Drug: Floxuridine|Drug: Leucovorin | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | Phase 1 | 1997-07-01 | 2008-03-03 |
NCT00005860 | Cancer | Drug: floxuridine|Drug: leucovorin calcium|Drug: oxaliplatin | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) | Phase 1 | 2000-04-01 | 2011-04-23 |
NCT00587067 | Hepatic Cancer | Drug: FLOXURIDINE | Memorial Sloan Kettering Cancer Center|Wake Forest University | Phase 2 | 2003-06-01 | 2017-02-06 |
NCT01938729 | Intrahepatic Cholangiocarcinoma|Peripheral Cholangiocarcinoma|Cholangiolar Carcinoma|Cholangiocellular Carcinoma) (ICC) | Procedure: Liver resection and placement of hepatic artery infusion pump|Drug: FLOXURIDINE|Drug: DEXAMETHASONE|Drug: GEMCITABINE | Memorial Sloan Kettering Cancer Center|Ohio State University|University of Texas Southwestern Medical Center|Washington University School of Medicine | Phase 1 | 2013-09-01 | 2016-09-09 |
NCT00492999 | Colorectal Cancer|Metastatic Cancer | Drug: dexamethasone|Drug: floxuridine|Drug: fluorouracil|Drug: irinotecan hydrochloride|Drug: leucovorin calcium|Drug: oxaliplatin | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) | Phase 2 | 2007-05-01 | 2016-06-01 |
NCT00002842 | Colorectal Cancer|Metastatic Cancer | Drug: floxuridine|Drug: fluorouracil|Drug: leucovorin calcium|Procedure: adjuvant therapy|Procedure: conventional surgery | City of Hope Medical Center|National Cancer Institute (NCI) | Phase 2 | 1994-09-01 | 2015-06-03 |
NCT00003753 | Colorectal Cancer|Metastatic Cancer | Drug: dexamethasone|Drug: floxuridine|Drug: irinotecan hydrochloride|Procedure: adjuvant therapy|Procedure: conventional surgery | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) | Phase 2 | 1998-09-01 | 2013-06-20 |
NCT00410956 | Liver Cancer | Biological: bevacizumab|Drug: dexamethasone|Drug: floxuridine|Genetic: protein expression analysis|Other: flow cytometry|Other: immunoenzyme technique|Other: immunohistochemistry staining method|Other: immunologic technique|Other: laboratory biomarker analysis|Procedure: dynamic contrast-enhanced magnetic resonance imaging | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) | Phase 2 | 2007-05-01 | 2016-10-24 |
NCT00858338 | Gastric Cancer|Stomach Cancer | Procedure: Potentially curative surgery|Drug: Floxuridine (IP)|Procedure: Adjuvant Chemoradiation therapy | New York University School of Medicine|Food and Drug Administration (FDA) | Phase 2 | 2002-12-01 | 2016-03-10 |
NCT02102789 | Metastatic Colorectal Cancer | Drug: mFOLFOX6|Drug: HAI | Yuhong Li|Sun Yat-sen University | Phase 3 | 2014-03-01 | 2015-10-28 |
NCT00200200 | Hepatic Metastases|Colon Cancer|Rectal Cancer | Drug: Bevacizumab HAI plus systemic chemotherapy|Drug: HAI plus systemic chemotherapy | Memorial Sloan Kettering Cancer Center|Mount Sinai Hospital, New York|Icahn School of Medicine at Mount Sinai | Phase 2 | 2004-11-19 | 2017-02-13 |
NCT00004142 | Colorectal Cancer|Metastatic Cancer | Drug: Floxuridine|Drug: Fluorouracil (5-FU)|Procedure: Conventional surgery|Procedure: Radiofrequency ablation | M.D. Anderson Cancer Center|National Cancer Institute (NCI) | Phase 2 | 1999-09-01 | 2012-07-27 |
NCT00645710 | Liver Metastases|Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IV Colon Cancer|Stage IV Rectal Cancer | Drug: gemcitabine hydrochloride|Drug: floxuridine|Genetic: proteomic profiling|Other: matrix-assisted laser desorption/ionization time of flight mass spectrometry|Other: liquid chromatography|Radiation: yttrium Y 90 anti-CEA monoclonal antibody cT84.66|Other: laboratory biomarker analysis|Other: mass spectrometry|Other: pharmacological study | City of Hope Medical Center | Phase 1|Phase 2 | 2005-02-01 | 2016-11-04 |
NCT01692704 | Cholangiocellular Carcinoma | Drug: Selective intra-arterial floxuridine and systemic gemcitabine and cisplatin | University of Zurich | Phase 1|Phase 2 | 2012-04-01 | 2016-03-24 |
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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