的影响一个人的细胞色素CYP3A4活性多烯紫杉醇间隙。

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Hirth J,沃特金斯PB, Strawderman M, Schott,布鲁诺R,贝克LH

的影响一个人的细胞色素CYP3A4活性多烯紫杉醇间隙。

癌症研究杂志2000年4月,6 (4):1255 - 8。

PubMed ID

10778948 (在PubMed

]

文摘

多烯紫杉醇是一种化学治疗剂有效的各种实体肿瘤的治疗。患者给予标准剂量的多烯紫杉醇展览宽interpatient间隙的变化(CL)和毒性作用。多西他赛经历由细胞色素CYP3A4代谢。因此,interpatient CYP3A4活动变化的差异也许可以解释部分毒性和CL。21严重预防转移性肉瘤患者接受多西他赛(100 mg / m2)。在每个病人测量肝CYP3A4活性[14 c-n-methyl]红霉素呼气试验(ERMBT)。血液样本被选中的时候在未来24小时进行药代动力学分析。表型的表达肝ERMBT CYP3A4活性测量的变化超过20倍(14 c呼出管理1 h:意思是,2.53%;范围0.25 - -5.35%),这是类似于一个正常的控制人口。CL多烯紫杉醇的多样的近6倍(意思是,21.0升/小时/平方米; range, 5.4-29.1 liters/h/m2). The ERMBT was the best predictor of CL when compared with serum alanine aminotransferase, albumin, alkaline phosphatase, or serum alpha-1-acidic glycoprotein. The natural log of ERMBT accounted for 67% of the interpatient variation in CL. Multivariate analysis showed that the natural log of ERMBT and albumin together accounted for 72% of the interpatient variation in CL. The greatest toxicity was seen in patients with the lowest ERMBT. Hepatic CYP3A4 activity is the strongest predictor of docetaxel CL and accounts for the majority of interpatient differences in CL. Patients with low CYP3A4 activity are at risk for having decreased CL and may thus experience increased toxicity from docetaxel. Those with high activity may be receiving a suboptimal dose. By measuring CYP3A4 activity, the ERMBT may be clinically useful in tailoring doses of CYP3A4 substrates, such as docetaxel, in certain individuals.

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药物酶

药物	酶	类	生物	药理作用	行动
多烯紫杉醇	细胞色素P450 3 a4	蛋白质	人类	未知的	底物 抑制剂	细节