他克莫司的药物基因组学研究进展
摘要
<正>他克莫司(tacrolimus,FK506)是从链霉菌属中分离出的一种新型强效免疫抑制药,它与环孢素(cyclosporine,CsA)同属于钙调磷酸酶抑制药(calcineurin inhibitors,CNIs)家族,由于其具有更好的免疫抑制作用和肝肾安全性,FK506正逐渐取代CsA成为器官移植患者术后的首选免疫抑制药。然而同CsA一样,FK506治疗窗窄、药动学个体差异大一直是困扰该药临床应用的难题,而编码药物代谢酶、药物转运体和药物作用靶点的基因序列的不同是引起
引文
1中华医学会器官移植学会肾移植组.他克莫司在临床肾移植中的应用指南[j].中华器官移植杂志,2010,31(9);565-562
2 Kamdem LK,Streit F,Zanger UM,et al.Contribution of CYP3A5 to the in vitro heputic clearance of lacrolimus[J].Clin Chem,2005;51(8):1374-1381
3 Bombail V,Taylor K,Gibson GG,et al.Role of Sp1,C/EBP alpha,HNF3,and PXR in the basal-and xenobiotic-mediated regulation of the CYP3A4 gene[J].Drug Metal,Dispos,2004;32:525-535
4 Azarpira N,Aghdaie MH,Behzad-Behbahonie A,et al.Association between cyclosporine concentration and genetic polymorphisms of CYP3A5 and MDR1 during the early stage after renal transplantation[J].Exp Clin Transplant,2006,4(1):416-419
5 Kamdem LK,Streit F,Zanger UM,et al.Contribution of CYP3A5 to the in vitro hepatic clearance of tacrolimus[J].Clin Chem,2005;51:1374-1381
6 Ball SE,Scatina J,Kao J,et al.Population distribution and effects on drug metabolism of a genetic variant in the 5'promoter region of CYP3A4[J].Clin Pharmacol Ther,1999,66(3):288
7 Hesselink DA,van Schaik RH.van der Heiden IP,et al.Genetic polymorphisms of the CYP3A4,CYP3A5,and MDR-I genes and pharmacokinetics of the calcineurin inhibitors cyclosporine and tacrolimus[J].Clin Pharmacol Ther,2003,74(3):245-254
8 Roy JN,Baramn A,Poirier C,et al.CYP3A4,CYP3A5.and MDR-1 genetic influences on lucrolimus pharmacokinetics in renal transplant recipienls[J].Phnrmacogenet Genomics,2006,16(9):659-665
9朱琳,宋洪涛,王庆华,等.CYP3A4*18B和CYP3A5*3基因多态性对肾移植患者他克莫司剂量及浓度的影响[J].药学学报,2012,47(7):878-883
10侯明明.侯颖,宋洪涛,等.肾移植患者CYP3A4基因多态性对他克莫司疗效和不良反应的影响[J].中国药房,2010.21(26):2427-2429
11李丹滢,陈燕华,方芸.CYP3A4/5单倍体将影响他克莫司血药谷浓度[C].2012.四川成都,第13次临床药理大会论文汇编,149-153
12 Shi XJ,Geng F,Jiao Z,et al.Association of ABCB1,CYP3A4*18B and CYP3A5*3 genotypes with the pharmacokinetics of tacrolimus in healthy Chinese subjects:a population pharmacokinetic analysis[J].Clin Pharm Ther,2011,36(5):614-624
13 Albekairy A,Alkatheri A,Fujita S,et al.Cytochrome P4503 A4FNx011B as pharmacogenomic predictor of tacrolimus pharmacokinetics and clinical outcome in the liver transplant recipients[J]..Saudi J Gastroenterol,2013,19(2):89-90
14 Larriba J,Imperiali N,Groppa R,et al.Pharmacogenetics of immunosuppressant polymorphism of CYP3A5 in renal transplant recipients[J].Trans Proceed,2010,42:257-259
15 Kuehl P,Zhang J,Lin Y,el al.Sequence diversity in CYP3A promoters and characterization of the genetic basis of polymorphic CYP3A5 expression[J].Nat Gene,2001,27(4),383-391
16 Staatz CE,Goodman LK.Tett SE.Effect of CYP3A and ABCB1 single nucleotide polymorphisms on the pharmacokinetics and pharmacodynamics of calcineurin inhibitors:Part I[J].Clin Pharmacokinet,2010,49(3):141-175
17王明丽.吴萍,罗光华.等.CYP3A基因多态性与他克莫司血药浓度的相关性研究[J].中国药房,2010,21(46):4343-4346
18吕慧怡,范青,马辉,等.CYP3A5基因多态性分析指导肾移植术后他克英司的个体化用药[J].中国医院药学杂志,2010,30(4):280-283
19张海燕,张小明,吴小丽.等.CYP3A5基因多态性对中国肾移植受者他克莫司血药浓度和疗效的影响[j].器官移植.2011,2(6):328-331
20侯明明,宋洪涛,王庆华,等。肾移植患者CYP3A5*3基因多态性对他克莫司血药浓度/剂量比和疗效的影响[J].中国医院药学杂志.2010,30(4):313-316
21 Provenzani A,Notarbartolo M,Labbozzetta M,et al.Influence of CYP3A5 and ABCB1 gene polymorphisms and other factors on tacrolimus dosing in Caucasian liver and kidney transplant patients[J],Int J Mol Med,2011,28(6):1093-1102
22 Katsakiori PF,Papapetrou EP,Sakellaropoulos GC.et al.Factors affecting the long-term response to tacrolimus in renal transplant patients;pharmacokinetic and pharmacogenetic approach[J].Int J Med Sci,2010,7(2):94-100
23石磊,保泽庆.朱云松,等.CYP3A5基因多态性与肾移植后钙调神经蛋白抑制剂慢性肾毒性的相关性[J].中国组织工程研究与临床康复.2011,15(5):806-809
24方洁,陈冰,张伟霞,等.肝移植中他克莫司血药浓度与多药耐药基因多态性的关系[J].中国临床药学杂志,2009,18(2):65-69
25刘其雨,李立.李晓延,等.ABCBI基因多态性对肝移植后他克莫司用量的影响[J].中国组织工程研究与临床康复,2011,15(31):5717-6721
26 Mendes J,Martinlio A,Simoes O,et al.Genetic polymorphisms in CYP3A5 and MDR1 genes and their correlations with plasma levels of tacrolimus and cyclosporine in renal transplant recipients[J].Transplantation Proceedings,2009,41(3):840-842
27 Yamauchi A,Leiri I,Kataoka Y,et al.Neurotoxicity indiced by tacrolimus after liver transplantation;relation to genetic polymorphisms of the ABCBI(MDR1)gene[J].Transplantation,2002,74(4):571-578
28 Wang J,Adriana Z,Kenneth M,et al.Impact of ABCBI(MDR1)haplotypes on tacrolimus dosing in adult lung transplant patients who are CYP3A5*3/*3 nonexpressors[J].Transplant Immunology,2006,15(3):235-240
29 Benkali K,Premaud A,Picard N,et al.Tacrolimus population pharmacokinetic-pharmacogenetic analysis and Bayesian estimation in renal transplant recipienls[J].Clin Pharmacokinet,2009,48(12):805-816
30 Press RR,Ploeger BA,den Hartigh J,et al.Explaining variability in tacrolimus pharmacokinetics to optimize early exposure in adult kidney transplant recipients[J].Therapeutic Drug Monitoring,2009,31(2):187-197
31 Elens L,Capron A,Kerckhove VV,et al.1199G>A and 2677G>T/A polymorphisms of ABCBI independently affect tacrolimus concentration in hepatic tissue after liver transplantation[J].Pharmacogenetics and Genomics,2007;17:873-888
32王金平,李澎灏,李雯.基于孕烷x受体基因多态性指导肾移植受者他克奠司的个体化用药[J].中国药房.2013.24(22):2049-2050
33 Li D,Zhu JY,Gao J,et al.Polymorphisms of tumor necrosis factor-α,interleukin-10,cytochromeP450 3A5 and ABCBI in Chinese liver transplant patients treated with immunosuppressant tacrolimus[J].Clinica Chimica Acta,2007,383(1-2):133-139
2 Kamdem LK,Streit F,Zanger UM,et al.Contribution of CYP3A5 to the in vitro heputic clearance of lacrolimus[J].Clin Chem,2005;51(8):1374-1381
3 Bombail V,Taylor K,Gibson GG,et al.Role of Sp1,C/EBP alpha,HNF3,and PXR in the basal-and xenobiotic-mediated regulation of the CYP3A4 gene[J].Drug Metal,Dispos,2004;32:525-535
4 Azarpira N,Aghdaie MH,Behzad-Behbahonie A,et al.Association between cyclosporine concentration and genetic polymorphisms of CYP3A5 and MDR1 during the early stage after renal transplantation[J].Exp Clin Transplant,2006,4(1):416-419
5 Kamdem LK,Streit F,Zanger UM,et al.Contribution of CYP3A5 to the in vitro hepatic clearance of tacrolimus[J].Clin Chem,2005;51:1374-1381
6 Ball SE,Scatina J,Kao J,et al.Population distribution and effects on drug metabolism of a genetic variant in the 5'promoter region of CYP3A4[J].Clin Pharmacol Ther,1999,66(3):288
7 Hesselink DA,van Schaik RH.van der Heiden IP,et al.Genetic polymorphisms of the CYP3A4,CYP3A5,and MDR-I genes and pharmacokinetics of the calcineurin inhibitors cyclosporine and tacrolimus[J].Clin Pharmacol Ther,2003,74(3):245-254
8 Roy JN,Baramn A,Poirier C,et al.CYP3A4,CYP3A5.and MDR-1 genetic influences on lucrolimus pharmacokinetics in renal transplant recipienls[J].Phnrmacogenet Genomics,2006,16(9):659-665
9朱琳,宋洪涛,王庆华,等.CYP3A4*18B和CYP3A5*3基因多态性对肾移植患者他克莫司剂量及浓度的影响[J].药学学报,2012,47(7):878-883
10侯明明.侯颖,宋洪涛,等.肾移植患者CYP3A4基因多态性对他克莫司疗效和不良反应的影响[J].中国药房,2010.21(26):2427-2429
11李丹滢,陈燕华,方芸.CYP3A4/5单倍体将影响他克莫司血药谷浓度[C].2012.四川成都,第13次临床药理大会论文汇编,149-153
12 Shi XJ,Geng F,Jiao Z,et al.Association of ABCB1,CYP3A4*18B and CYP3A5*3 genotypes with the pharmacokinetics of tacrolimus in healthy Chinese subjects:a population pharmacokinetic analysis[J].Clin Pharm Ther,2011,36(5):614-624
13 Albekairy A,Alkatheri A,Fujita S,et al.Cytochrome P4503 A4FNx011B as pharmacogenomic predictor of tacrolimus pharmacokinetics and clinical outcome in the liver transplant recipients[J]..Saudi J Gastroenterol,2013,19(2):89-90
14 Larriba J,Imperiali N,Groppa R,et al.Pharmacogenetics of immunosuppressant polymorphism of CYP3A5 in renal transplant recipients[J].Trans Proceed,2010,42:257-259
15 Kuehl P,Zhang J,Lin Y,el al.Sequence diversity in CYP3A promoters and characterization of the genetic basis of polymorphic CYP3A5 expression[J].Nat Gene,2001,27(4),383-391
16 Staatz CE,Goodman LK.Tett SE.Effect of CYP3A and ABCB1 single nucleotide polymorphisms on the pharmacokinetics and pharmacodynamics of calcineurin inhibitors:Part I[J].Clin Pharmacokinet,2010,49(3):141-175
17王明丽.吴萍,罗光华.等.CYP3A基因多态性与他克莫司血药浓度的相关性研究[J].中国药房,2010,21(46):4343-4346
18吕慧怡,范青,马辉,等.CYP3A5基因多态性分析指导肾移植术后他克英司的个体化用药[J].中国医院药学杂志,2010,30(4):280-283
19张海燕,张小明,吴小丽.等.CYP3A5基因多态性对中国肾移植受者他克莫司血药浓度和疗效的影响[j].器官移植.2011,2(6):328-331
20侯明明,宋洪涛,王庆华,等。肾移植患者CYP3A5*3基因多态性对他克莫司血药浓度/剂量比和疗效的影响[J].中国医院药学杂志.2010,30(4):313-316
21 Provenzani A,Notarbartolo M,Labbozzetta M,et al.Influence of CYP3A5 and ABCB1 gene polymorphisms and other factors on tacrolimus dosing in Caucasian liver and kidney transplant patients[J],Int J Mol Med,2011,28(6):1093-1102
22 Katsakiori PF,Papapetrou EP,Sakellaropoulos GC.et al.Factors affecting the long-term response to tacrolimus in renal transplant patients;pharmacokinetic and pharmacogenetic approach[J].Int J Med Sci,2010,7(2):94-100
23石磊,保泽庆.朱云松,等.CYP3A5基因多态性与肾移植后钙调神经蛋白抑制剂慢性肾毒性的相关性[J].中国组织工程研究与临床康复.2011,15(5):806-809
24方洁,陈冰,张伟霞,等.肝移植中他克莫司血药浓度与多药耐药基因多态性的关系[J].中国临床药学杂志,2009,18(2):65-69
25刘其雨,李立.李晓延,等.ABCBI基因多态性对肝移植后他克莫司用量的影响[J].中国组织工程研究与临床康复,2011,15(31):5717-6721
26 Mendes J,Martinlio A,Simoes O,et al.Genetic polymorphisms in CYP3A5 and MDR1 genes and their correlations with plasma levels of tacrolimus and cyclosporine in renal transplant recipients[J].Transplantation Proceedings,2009,41(3):840-842
27 Yamauchi A,Leiri I,Kataoka Y,et al.Neurotoxicity indiced by tacrolimus after liver transplantation;relation to genetic polymorphisms of the ABCBI(MDR1)gene[J].Transplantation,2002,74(4):571-578
28 Wang J,Adriana Z,Kenneth M,et al.Impact of ABCBI(MDR1)haplotypes on tacrolimus dosing in adult lung transplant patients who are CYP3A5*3/*3 nonexpressors[J].Transplant Immunology,2006,15(3):235-240
29 Benkali K,Premaud A,Picard N,et al.Tacrolimus population pharmacokinetic-pharmacogenetic analysis and Bayesian estimation in renal transplant recipienls[J].Clin Pharmacokinet,2009,48(12):805-816
30 Press RR,Ploeger BA,den Hartigh J,et al.Explaining variability in tacrolimus pharmacokinetics to optimize early exposure in adult kidney transplant recipients[J].Therapeutic Drug Monitoring,2009,31(2):187-197
31 Elens L,Capron A,Kerckhove VV,et al.1199G>A and 2677G>T/A polymorphisms of ABCBI independently affect tacrolimus concentration in hepatic tissue after liver transplantation[J].Pharmacogenetics and Genomics,2007;17:873-888
32王金平,李澎灏,李雯.基于孕烷x受体基因多态性指导肾移植受者他克奠司的个体化用药[J].中国药房.2013.24(22):2049-2050
33 Li D,Zhu JY,Gao J,et al.Polymorphisms of tumor necrosis factor-α,interleukin-10,cytochromeP450 3A5 and ABCBI in Chinese liver transplant patients treated with immunosuppressant tacrolimus[J].Clinica Chimica Acta,2007,383(1-2):133-139