| 他克莫司的药物基因组学与个体化用药 |
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| 引用本文： | 朱琳,华之卉,宋洪涛. 他克莫司的药物基因组学与个体化用药[J]. 中国临床药理学与治疗学, 2011, 16(6): 710-715 |
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| 作者姓名： | 朱琳 华之卉 宋洪涛 |
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| 作者单位： | 1. 南京军区福州总医院药学科,福州350025,福建;沈阳药科大学药学院,沈阳110016,辽宁
2. 南京军区福州总医院药学科,福州350025,福建 |
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| 摘 要： | 他克莫司(FK506)是一种广泛应用的免疫抑制剂,在器官移植中发挥重要作用,由于治疗窗窄、个体间差异较大,常需要进行治疗药物监测。FK506是CYP3A酶和药物转运体P-糖蛋白(P-gp)的底物,CYP3A酶参与FK506的代谢而P-gp参与FK506的转运。这些酶的表达水平及生物活性差异可能会导致FK506个体间差异,而CYP3A及多药耐药基因(MDR1)基因多态性可能会影响CYP3A酶及P-gp的生物活性,所以CYP3A与MDR1基因多态性可能是造成FK506个体间差异的重要原因。本文就近年来FK506的药物基因组学研究进展加以综述。
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| 关 键 词： | 他克莫司 基因多态性 CYP3A4 CYP3A5 多药耐药基因 |
Pharmacogenomics and personalized medicine of tacrolimus |
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| ZHU Lin,HUA Zhi-hui,SONG Hong-tao. Pharmacogenomics and personalized medicine of tacrolimus[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2011, 16(6): 710-715 |
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| Authors: | ZHU Lin HUA Zhi-hui SONG Hong-tao |
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| Affiliation: | ZHU Lin1,2,HUA Zhi-hui1,SONG Hong-tao11Department of Pharmacy,Fuzhou General Hospital of Nanjing Military Region,Fuzhou 350025,Fujian,China,2Department of Pharmaceutics,School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,Liaoning |
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| Abstract: | Tacrolimus(FK506),a widely used immunosuppressant,exerts a key effect in patients with organ transplantation.The drug requires therapeutic monitoring due to its narrow therapeutic index and great inter-individual variability.FK506 is known to be a substrate of CYP3A and P-glycoprotein(P-gp).FK506 is metabolized by CYP3A and transported by P-gp.The difference in expression level and the bioactivity of these proteins may explain individual variations of FK506 pharmacokinetics.The differences in bioactivities ... |
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| Keywords: | Tacrolimus Gene polymorphism CYP3A4 CYP3A5 MDR1 |
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