Gimeracil是二氢嘧啶脱氢酶(DPYD)抑制剂,能降解血液中的包含5-fluorouracil等的嘧啶。
Gimeracil is an inhibitor of dihydropyrimidine dehydrogenase, which inhibits the early step in homologous recombination for double strand breaks repair.
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] Petra Matt, et al. Oncologist. 2011 Oct; 16(10): 1451–1457. Published online 2011 Sep 30. doi:10.1634/theoncologist.2011-0224.
[2] Makoto Tahara,et al. Cancer Sci. 2015 Oct; 106(10): 1414–1420. Published online 2015 Sep 21. doi: 10.1111/cas.12764.
分子式 C5H4ClNO2 |
分子量 145.54 |
CAS号 103766-25-2 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 29 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 |
NCT01492543 | Breast Cancer | Drug: Tegafur Gimeracil Oteracil Potassium Capsule | Chinese Academy of Medical Sciences|Beijing Cancer Hospital|Beijing Chao Yang Hospital|Chinese PLA General Hospital|China-Japan Friendship Hospital|Tianjin Medical University Cancer Institute and Hospital|Hebei Tumor Hospital | Phase 2 | 2011-12-01 | 2013-03-14 |
NCT01516944 | Gastric Cancer | Drug: Tegafur, Gimeracil and Oteracil Potassium Capsulesxaliplatin|Drug: Tegafur, Gimeracil and Oteracil Potassium Capsulesxaliplatin|Drug: Oxaliplatin; Capecitabine | Hebei Medical University | Phase 2|Phase 3 | 2012-02-01 | 2016-09-04 |
NCT01285557 | Metastatic Diffuse Gastric Cancer Including Carcinoma of the Gastro-esophageal Junction | Drug: S-1 (Tegafur/Gimeracil/Oteracil) /cisplatin (investigational arm)|Drug: Fluorouracil/cisplatin (control arm) | Taiho Oncology, Inc. | Phase 3 | 2011-02-01 | 2016-10-19 |
NCT02008422 | Gastric Cancer | Drug: Oxaliplatin|Drug: Gimeracil and Oteracil Potassium Capsule|Drug: Endostar injection | Tang Xushan|Xinjiang Medical University | Phase 3 | 2013-08-01 | 2013-12-06 |
NCT02504229 | Gastric Cancer | Biological: autologous dendritic cells co-cultured with cytokine-induced killer cells|Drug: Gimeracil and Oteracil Porassium Capsules|Drug: Oxaliplatin | Beijing Biohealthcare Biotechnology Co.,Ltd | Phase 2 | 2014-11-01 | 2015-07-20 |
NCT02024217 | Gastric Cancer | Radiation: S1xaliplatinadiation | Fudan University | Phase 2 | 2012-03-01 | 2013-12-25 |
NCT00660894 | Colorectal Cancer | Drug: folinate calcium|Drug: tegafur-uracil|Drug: tegafur-gimeracil-oteracil potassium | Translational Research Informatics Center, Kobe, Hyogo, Japan | Phase 3 | 2008-04-01 | 2016-08-02 |
NCT03006705 | Gastric Cancer | Drug: ONO-4538|Drug: Tegafur-gimeracil-oteracil potassium|Drug: Oxaliplatin|Drug: Capecitabine|Drug: Placebo | Ono Pharmaceutical Co. Ltd|Bristol-Myers Squibb | Phase 3 | 2017-01-01 | 2017-03-21 |
NCT03002831 | Advanced Cancer | Biological: Cytokine-induced Killer Cells|Drug: Tegafur-Gimeracil-Oteracil Potassium | Henan Cancer Hospital | Phase 2 | 2016-11-01 | 2016-12-23 |
NCT01655992 | Metastatic Breast Cancer | Drug: capecitabine|Drug: S1 generic | Fudan University | Phase 3 | 2012-01-01 | 2017-01-03 |
NCT02746796 | Gastric Cancer | Drug: ONO-4538|Drug: Oxaliplatin|Drug: Tegafur- Gimeracil-Oteracil potassium|Drug: Capecitabine|Drug: Placebo | Ono Pharmaceutical Co. Ltd | Phase 2|Phase 3 | 2016-03-01 | 2017-02-28 |
NCT00503321 | Gastric Cancer | Drug: Tegafur/gimeracil/oteracil potassium (S-1), Krestin (PSK)|Drug: Tegafur/gimeracil/oteracil potassium (S-1) | Eastern Network of Cancer Immunological Therapy, Japan | Phase 2|Phase 3 | 2006-10-01 | 2009-01-22 |
NCT02277158 | Rectal Cancer | Drug: Chemoradiotherapy | Daping Hospital and the Research Institute of Surgery of the Third Military Medical University | Phase 1 | 2014-11-01 | 2014-11-30 |
NCT02618356 | Metastatic Colon Cancer | Drug: Raltitrexed and S-1 | Fudan University | Phase 2 | 2015-12-01 | 2015-12-02 |
NCT02945267 | Unresectable Pancreatic Cancer | Drug: Nimotuzumab plus S1|Drug: Placebo plus S1 | Chinese PLA General Hospital | Phase 4 | 2016-09-01 | 2016-10-25 |
NCT02527824 | Biliary Tract Neoplasm | Drug: Oxaliplatin, Irinotecan, S-1 | Hallym University Medical Center|Jeil Pharmaceutical Co., Ltd. | Phase 2 | 2015-03-01 | 2016-09-27 |
NCT02527785 | Stomach Neoplasm | Drug: Oxaliplatin, Irinotecan, S-1(OIS) | Hallym University Medical Center|Jeil Pharmaceutical Co., Ltd. | Phase 2 | 2015-02-01 | 2016-09-27 |
NCT03013010 | Stomach Neoplasm|GastroEsophageal Cancer|Adenocarcinoma|Locally Advanced Cancer|Chemoradiation | Drug: Tegafur-Gimeracil-Oteracil Potassium|Radiation: Chemoradiotherapy|Procedure: Gastric resection|Drug: Oxaliplatin | Shanghai Cancer Hospital, China|Fudan University|Ruijin Hospital|Xinhua Hospital, Shanghai Jiao Tong University School of Medicine|Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine|Huadong Hospital | Phase 3 | 2016-12-01 | 2017-01-04 |
NCT01388790 | Gastric Cancer | Drug: Cetuximab|Drug: Cisplatin|Drug: S-1 | Merck KGaA | Phase 2 | 2011-06-01 | 2013-09-09 |
NCT00974389 | Colorectal Cancer | Biological: bevacizumab|Drug: tegafur-gimeracil-oteracil potassium | Osaka Medical College|National Cancer Institute (NCI) | Phase 2 | 2009-07-01 | 2013-08-09 |
NCT00687843 | Gastric Cancer | Drug: Tegafur-gimeracil-oteracil potassium (TS-1)|Drug: Krestin (PSK) | Tokyo Metropolitan Oncology Group | Phase 3 | 2008-06-01 | 2012-03-20 |
NCT00216034 | Gastric Cancer | Drug: Tegafur-gimeracil-oteracil potassium (TS-1)|Drug: Krestin (PSK) | Hokuriku-Kinki Immunochemotherapy Study Group | Phase 3 | 2005-03-01 | 2016-06-06 |
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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