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首页> 外文期刊>Biomedical Chromatography: An International Journal Devoted to Research in Chromatographic Methodologies and Their Applications in the Biosciences >Development of a sensitive UHPLC-MS/MS method for the pharmacokinetics study of a novel tyrosine kinase inhibitors, 1-[4-(4-{5-Chloro-4-[2-(propane-2-sulfonyl)-phenylamino]-pyrimidin-2-ylamino}-phenyl)-piperazin-1-yl]-propenone in rats
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Development of a sensitive UHPLC-MS/MS method for the pharmacokinetics study of a novel tyrosine kinase inhibitors, 1-[4-(4-{5-Chloro-4-[2-(propane-2-sulfonyl)-phenylamino]-pyrimidin-2-ylamino}-phenyl)-piperazin-1-yl]-propenone in rats

机译：开发新型酪氨酸激酶抑制剂的药代动力学研究的敏感UHPLC-MS / MS方法，1- [4-（4-（4-（4-氯-4- [2-（丙烷-2-磺酰基） - 苯氨基] - 嘧啶-2- ylamino} -phenyl）-piperazin-1-基] - 大鼠丙酮

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Targeted inhibition of epidermal growth factor receptor has become an important means of chemotherapy for nonsmall cell lung cancer, breast cancer, pancreatic cancer, colon cancer and other malignant tumors. Although remarkable curative effects have been achieved in the past few decades, the emergence of drug resistance is a problem. Therefore, new inhibitors need to be developed. XHL-31 is a new candidate with significant inhibitory activity against T790M and C797S mutations in vitro. In order to study the pharmacokinetics in vivo, a sensitive and efficient UHPLC-MS/MS method was developed for the determination of XHL-31 in rat plasma in this study. The lower limit of quantitation of this method was 1 ng/ml and the linear range was 1-2,000 ng/ml. Method validation showed a high accuracy and precision, a high stability, a high recovery and repeatability. The method was successfully applied to the pharmacokinetic study of XHL-31 in rats. The results indicated that there were significant gender differences in oral absorption and the absolute bioavailability of XHL-31 in female rats were extremely low (< 10%).
机译：针对性生长因子受体的靶向抑制已成为Nonsmall细胞肺癌，乳腺癌，胰腺癌，结肠癌和其他恶性肿瘤的重要化疗的重要手段。虽然在过去的几十年里已经实现了显着的疗效，但耐药性的出现是一个问题。因此，需要开发新的抑制剂。 XHL-31是对T790M和体外C797S突变具有显着抑制活性的新候选者。为了研究体内的药代动力学，开发了敏感和有效的UHPLC-MS / MS方法，用于测定该研究大鼠血浆中的XHL-31。该方法的定量下限为1ng / ml，线性范围为1-2,000ng / ml。方法验证显示出高精度和精度，高稳定性，高回收率和重复性。该方法成功地应用于大鼠XHL-31的药代动力学研究。结果表明，口腔吸收方面存在显着性的性别差异，雌性大鼠XHL-31的绝对生物利用度极低（<10％）。

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