Folinic acid calcium

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Chemical Structure| 1492-18-8 同义名 : 亚叶酸钙 ;Leucovorin calcium;Calcium folinate;5-Formyltetrahydrofolate;NSC 3590;DL-Folinate;DL-Folinic Acid (calcium salt);Wellcovorin;Folinic acid calcium salt
CAS号 : 1492-18-8
货号 : A161719
分子式 : C20H21CaN7O7
纯度 : 95%
分子量 : 511.501
MDL号 : MFCD08704249
存储条件:

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

H2O: 50 mg/mL(97.75 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Calcium Folinate (CF) is a biological folic acid and is generally administered along with methotrexate (MTX) as a rescue agent to decrease MTX-induced toxicity. Endosalpingitis, the ultrastructural damage of endosalpinx, and a change in estrogen and P receptor expression induced by low- and high-dose MTX (methotrexate) in endosalpinx can be reversed completely and partly (B1, B2) by combined treatment with CF, suggesting that CF combined with MTX protects against the side effects induced by MTX[3]. Uracil and tegafur (UFT) plus calcium folinate are the components of the oral agent known as Orzel, which offers activity comparable to intravenously administered 5-fluorouracil (5-FU) combined with calcium folinate[4]. UFT (uracil and tegafur) plus oral calcium folinate (Orzel) offers significant antitumor activity and an acceptable toxicity profile makes this a logical formulation for the adjuvant treatment of colon cancer[5]. Furthermore, tegafur/uracil + calcium folinate is well tolerated, with dose-limiting toxicity manifesting as diarrhoea. Compared with intravenous fluorouracil plus folinic acid (leucovorin) regimens, tegafur/uracil + calcium folinate has similar efficacy with less toxicity and is more convenient because it is an oral regimen[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00591045 Stomach Neoplasms ... 展开 >> Gastric Cancer 收起 << Phase 2 Unknown December 2012 China, Beijing ... 展开 >> Peking University School of Oncology Not yet recruiting Beijing, Beijing, China, 100036 Contact: Jiafu Ji, M.D.    86-10-88196048    jiafuj@hotmail.com    Principal Investigator: Jiafu Ji, M.D. 收起 <<
NCT02573220 Stage IVA Colorectal Cancer ... 展开 >> Stage IVB Colorectal Cancer 收起 << Phase 1 Withdrawn(Study terminated by ... 展开 >>PI due to inability to accrue.) 收起 << - Italy ... 展开 >> Centro di Riferimento Oncologico Aviano, Italy, 33081 收起 <<
NCT00677287 Colorectal Cancer ... 展开 >> Colon Cancer Rectal Cancer 收起 << Phase 1 Phase 2 Terminated(Lack of financial s... 展开 >>upport) 收起 << - Japan ... 展开 >> The Institute of Medical Science, the University of Tokyo Minato-ku, Tokyo, Japan, 108-8639 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.96mL

0.39mL

0.20mL

9.78mL

1.96mL

0.98mL

19.55mL

3.91mL

1.96mL

参考文献

[1]Chang WN, Tsai JN, et al. Serine hydroxymethyltransferase isoforms are differentially inhibited by leucovorin: characterization and comparison of recombinant zebrafish serine hydroxymethyltransferases. Drug Metab Dispos. 2007 Nov;35(11):2127-37.

[2]Schilsky RL, Ratain MJ. Clinical pharmacokinetics of high-dose leucovorin calcium after intravenous and oral administration. J Natl Cancer Inst. 1990 Sep 5;82(17):1411-5.

[3]Yang XJ, Chen YP, Wang HC, Zhao J, Zheng FY. Protective effect of calcium folinate against methotrexate-induced endosalpinx damage in rats. Fertil Steril. 2011 Mar 15;95(4):1526-30

[4]Bokemeyer C, Hartmann JT, Kollmannsberger C, Mayer F, Kanz L. UFT/calcium folinate plus weekly paclitaxel for solid tumors. Oncology (Williston Park). 1999 Jul;13(7 Suppl 3):106-11

[5]Smith R, Wickerham DL, Wieand HS, Colangelo L, Mamounas EP. UFT plus calcium folinate vs 5-FU plus calcium folinate in colon cancer. Oncology (Williston Park). 1999 Jul;13(7 Suppl 3):44-7

[6]Hoff PM, Lassere Y, Pazdur R. Tegafur/uracil + calcium folinate in colorectal cancer: double modulation of fluorouracil. Drugs. 1999;58 Suppl 3:77-83