Raltitrexed是胸苷酸合成酶抑制剂,是肿瘤化疗中的抗代谢剂。
Raltitrexed is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth. Raltitrexed is a folate-based inhibitor of thymidylate synthase (TS) that is rapidly and extensively metabolized to its more potent polyglutamate derivatives. Raltitrexed is an inhibitor of DHFR.
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] Peters GJ, et al. Eur J Cancer, 2000, 36(7), 916-924.
[2] Jodrell, D I., et al., 1991. The pharmacokinetics of the quinazoline antifolate ICI D 1694 in mice and rats. Cancer chemotherapy and pharmacology. 28(5): 331-8.
[3] Jackman, A L., et al., . ZD1694 (Tomudex): a new thymidylate synthase inhibitor with activity in colorectal cancer. European journal of cancer (Oxford, England : 1990). 31A(7-8): 1277-82.
分子式 C21H22N4O6S |
分子量 458.49 |
CAS号 112887-68-0 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 90 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 |
NCT02618356 | Metastatic Colon Cancer | Drug: Raltitrexed and S-1 | Fudan University | Phase 2 | 2015-12-01 | 2015-12-02 |
NCT02562599 | Nasopharyngeal Carcinoma | Drug: raltitrexed-cisplatin|Radiation: Intensity-modulated radiotherapy (IMRT) | Hubei Cancer Hospital | Phase 2 | 2015-08-01 | 2015-09-28 |
NCT02557490 | Colon Cancer Liver Metastasis | Drug: oxaliplatin and raltitrexed | Zhu Xu|Beijing Cancer Hospital | Phase 4 | 2015-01-01 | 2015-09-22 |
NCT03053167 | ColoRectal Cancer | Drug: Irinotecan|Drug: Raltitrexed | China Medical University, China|The First Affiliated Hospital of Dalian Medical University|The Second Affiliated Hospital of Dalian Medical University|Liaoning Tumor Hospital & Institute|Shengjing Hospital|General Hospital of Shenyang Military Region | Phase 2 | 2016-12-01 | 2017-02-13 |
NCT03083613 | Gastric Cancer|Gastroesophageal Junction Adenocarcinoma | Drug: Raltitrexed|Drug: Paclitaxel | Chinese Academy of Medical Sciences | Phase 2 | 2015-05-01 | 2017-03-14 |
NCT02072317 | Advanced Gastric Cancer | Drug: taxel plus raltitrexed|Drug: taxol | Fudan University | Phase 2 | 2013-11-01 | 2014-02-24 |
NCT01836120 | Gastric Cancer | Drug: Raltitrexed plus Docetaxel|Drug: Docetaxel | Hebei Tumor Hospital | Phase 2 | 2013-04-01 | 2013-04-18 |
NCT00003528 | Recurrent Childhood Acute Lymphoblastic Leukemia|Recurrent Childhood Acute Myeloid Leukemia | Drug: raltitrexed | National Cancer Institute (NCI) | Phase 1 | 1998-09-01 | 2013-01-15 |
NCT01732380 | Inoperable Esophageal Cancer Stage I-III | Drug: Raltitrexed|Drug: Oxaliplatin|Radiation: Radiotherapy | The First People's Hospital of Lianyungang|The East Hospital of Lianyungang|Donghai People's Hospital|People's Hospital of Ganyu | Phase 2 | 2012-07-01 | 2012-11-19 |
NCT01959061 | Colorectal Cancer Metastatic | Drug: Raltitrexed|Drug: Oxaliplatin|Drug: lipiodol | Nanjing Chia-tai Tianqing Pharmaceutical | Phase 4 | 2013-09-01 | 2017-03-09 |
NCT02485548 | Head and Neck Squamous Cell Cancer | Drug: Raltitrexed|Drug: 5-fluorouracil|Drug: Cisplatin|Radiation: IMRT | Jiangsu Cancer Institute & Hospital|Wuxi Cancer Hospital|Changzhou Cancer Hospital|Nanjing Cancer Hospital|Northern Jiangsu Province People's Hospital|The Second Hospital of Nanjing Medical University|Nanjing BenQ Hospital | Phase 3 | 2015-06-01 | 2015-06-29 |
NCT02992886 | Rectal Neoplasms Malignant | Radiation: Preoperative radiation|Drug: Raltitrexed|Procedure: Pelvic surgery | Chinese Academy of Medical Sciences | Phase 2 | 2016-09-01 | 2016-12-13 |
NCT02821559 | Metastatic Colorectal Cancer | Drug: TOMOX|Drug: Bevacizumab | Centre Hospitalier Universitaire de Besancon|Hospira, Inc. | Phase 2 | 2012-07-01 | 2016-06-29 |
NCT00590278 | Inoperable or Recurrent Rectal Cancer | Drug: Tomudex|Procedure: Radiotherapy|Procedure: Haematology|Procedure: Biochemistry | AstraZeneca | Phase 2 | 2002-08-01 | 2008-01-23 |
NCT01348412 | Colorectal Cancer|Liver Metastases | Drug: oxaliplatin|Drug: raltitrexed|Drug: other intravenous chemotherapy drugs | Centre Georges Francois Leclerc|National Cancer Institute, France|Hospira, Inc. | Phase 2 | 2010-12-01 | 2016-04-22 |
NCT00234429 | Colorectal Cancer | Drug: Gefitinib, raltitrexed | AstraZeneca | Phase 2|Phase 3 | 2003-11-01 | 2007-12-14 |
NCT00004920 | Malignant Mesothelioma | Drug: cisplatin|Drug: raltitrexed | European Organisation for Research and Treatment of Cancer - EORTC | Phase 3 | 1999-11-01 | 2012-07-17 |
NCT02631564 | Colon Cancer Liver Metastasis | Fudan University | 2015-06-01 | 2015-12-14 | ||
NCT00002828 | Colorectal Cancer | Drug: fluorouracil|Drug: raltitrexed | Memorial Sloan Kettering Cancer Center | Phase 1 | 1995-04-01 | 2013-06-20 |
NCT02453490 | Colorectal Cancer|Liver Metastasis | Drug: Raltitrexed-based chemotherapy|Drug: Raltitrexed-based chemotherapy|Drug: 5-fluorouracil-based chemotherapy|Drug: 5-fluorouracil-based chemotherapy | Zhejiang University | Phase 3 | 2015-10-01 | 2017-03-10 |
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。
相关化合物库
使用AMQUAR产品发表文献后请联系我们