Abiraterone acetate efficacy against prostate cancer is dependent on the circulating levels of abiraterone and its active metabolites, which present significant pharmacokinetic variability among patients. Thus, therapeutic drug monitoring can be performed to improve treatment outcomes. To support such studies, there are only a limited number of bioanalytical methods in current literature. This work presents a fast method to quantify abiraterone and D4A in plasma in 4 min by UPLC–MS/MS. Bioanalytical method validation was performed according to the recommendations of the US Food and Drug Administration. The method was linear within the range of 1–400 ng/ml for abiraterone and 0.2–20 ng/ml for D4A (r² > 0.99). Based on the analysis of quality control samples at the lower limit of quantification, low, medium and high concentrations, the method was precise (CV_abiraterone ≤ 9.72%; CV_D4A ≤ 14.64%) and accurate (CV_abiraterone 95.51–107.59%; CV_D4A 98.04–99.89%). Application of the method to the quantification of abiraterone and D4A in 10 clinical samples revealed important variability in the conversion ratio of abiraterone to D4A (CV 90.85%). Considering the current literature, this is the fastest method to quantify abiraterone and D4A in plasma, allowing for optimization of the analytical routine.

中文翻译：

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一种快速的UPLC-MS / MS方法，用于在人血浆中监测阿比特龙和δ（4）-阿比特龙的治疗药物。

乙酸阿比特龙酯对前列腺癌的功效取决于阿比特龙及其活性代谢物的循环水平，阿比特龙及其活性代谢物在患者之间呈现出显着的药代动力学变异性。因此，可以执行治疗药物监测以改善治疗效果。为了支持这样的研究，当前文献中仅有有限数量的生物分析方法。这项工作提出了一种通过UPLC-MS / MS在4分钟内定量测定血浆中阿比特龙和D4A的快速方法。根据美国食品和药物管理局的建议进行了生物分析方法验证。该方法在阿比特龙的1-400 ng / ml和D4A的0.2-20 ng / ml范围内是线性的（r ² > 0.99）。基于质量控制样品的定量，低，中，高浓度的下限的分析，该方法是精确的（CV_阿比特龙 ≤9.72％; CV _D4A  ≤14.64％）和精确（CV_阿比特龙95.51-107.59％; CV _D4A 98.04–99.89％）。该方法在10个临床样品中对阿比特龙和D4A定量的应用表明，阿比特龙对D4A的转化率具有重要的差异（CV 90.85％）。考虑到当前文献，这是定量血浆中阿比特龙和D4A的最快方法，可优化分析程序。