Abstract：
Background: SYHA1807 is a novel lysine specific demethylase 1 inhibitor being developed for the treatment of small-cell lung cancer. Aim: This study aimed to establish a ultra-performance liquid chromatography-mass spectrometry (UPLC-MS)/MS method for measuring SYHA1807 in human plasma, supporting its application in a first-in-human study. Methods: SYHA1807 was separated on an ACQUITY UPLC BEH® C18 Column (2.1 × 50 mm, 1.7 μm) after protein precipitation of plasma samples. Mass spectrometry analysis was performed with a Xevo TQS triple quadrupole mass spectrometer utilizing a positive electronic spray ionization source. The established method was fully validated according to bioanalytical guidelines. Results & conclusion: A rapid, specific and robust UPLC-MS/MS method was first established for quantifying SYHA1807 and successfully applied in a first-in-human study.
摘要：
背景：SYHA1807是一种新的赖氨酸特异性脱甲基酶1抑制剂，正在开发用于治疗小细胞肺癌。目的:建立超高效液相色谱-质谱(UPLC-MS)/MS法测定人血浆中SYHA1807,支持其在首次人体研究中的应用。方法：在ACQUITYUPLCBEH®C18色谱柱上分离SYHA1807（2.1×50mm，1.7μm）在血浆样品的蛋白质沉淀后。使用XevoTQS三重四极杆质谱仪利用正电子喷雾电离源进行质谱分析。根据生物分析指南对所建立的方法进行了充分验证。结果与结论：快速，首次建立了特异性和稳健的UPLC-MS/MS方法来定量SYHA1807，并成功应用于首次人体研究。
