液相色谱-串联质谱法测定人血浆中恩杂鲁胺及其主要代谢物含量的方法验证
Validation of a method for quantifying enzalutamide and its major metabolites in human plasma by LC-MS/MS.
作者信息
Bennett Daniel, Gibbons Jacqueline A, Mol Roelof, Ohtsu Yoshiaki, Williard Clark
机构信息
inVentiv Health Clinical Lab, Inc, 301D College Road East, Princeton, NJ 08540, USA.
出版信息
Bioanalysis. 2014 Mar;6(6):737-44. doi: 10.4155/bio.13.325. Epub 2013 Dec 12.
BACKGROUND
Enzalutamide is an androgen receptor inhibitor that targets multiple steps in the androgen receptor signaling pathway. Oral enzalutamide was recently approved by the US FDA and health authorities in other regions for the treatment of patients with metastatic castration-resistant prostate cancer who previously received docetaxel. The objective of this study was to validate a method for quantification of enzalutamide and its two major metabolites in human plasma.
RESULTS
The analytes were extracted from plasma by an LLE procedure, separated by reversed phase HPLC and detected by MS/MS in positive mode ESI. The quantitation range was 0.0200-50.0 µg/ml.
CONCLUSION
The method proved to be rapid and simple, and met FDA validation criteria.
背景
恩杂鲁胺是一种雄激素受体抑制剂，作用于雄激素受体信号通路的多个环节。口服恩杂鲁胺最近已获美国食品药品监督管理局（FDA）及其他地区卫生当局批准，用于治疗既往接受过多西他赛治疗的转移性去势抵抗性前列腺癌患者。本研究的目的是验证一种定量测定人血浆中恩杂鲁胺及其两种主要代谢物的方法。
结果
采用液液萃取（LLE）法从血浆中提取分析物，经反相高效液相色谱（HPLC）分离，采用电喷雾电离（ESI）正离子模式下的串联质谱（MS/MS）检测。定量范围为0.0200 - 50.0μg/ml。
结论
该方法快速简便，符合FDA的验证标准。
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