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Zhou, Sufeng; Liu, Wei; Zhou, Chen; Zhang, Lingling; Xie, Lijun; Xu, Zhaoqiang; Wang, Lu; Zhao, Yuqing; Guo, Lian; Chen, Juan; Ding, Lieming; Mao, Li; Tao, Yi; Zhang, Chen; Ding, Sijia; Shao, Feng
Cancer chemotherapy and pharmacology, 12/2020, Volume: 86, Issue: 6Journal Article
Purpose Ensartinib is a novel, potent and highly selective inhibitor of anaplastic lymphoma kinase (ALK) that has promising clinical activity and low toxicity in patients with ALK-positive non-small cell lung cancer. This study was conducted to investigate the pharmacokinetics, metabolism and excretion of ensartinib following a single 200 mg/100 μCi oral dose of radiolabeled ensartinib to healthy subjects. Methods Six healthy male subjects were enrolled and administrated an oral suspension in a fasted state. Blood, urine and feces were collected. Radioactivity concentrations were measured by liquid scintillation counting and plasma concentrations of ensartinib by liquid chromatography-tandem mass spectrometry. Both techniques were applied for metabolite profiling and characterization. Results The mean total recovery was 101.21% of the radiolabeled dose with 91.00% and 10.21% excreted in feces and urine, respectively. Unchanged ensartinib was the predominant drug-related component in urine and feces, representing 4.39% and 38.12% of the administered dose, respectively. Unchanged ensartinib and its metabolite M465 were the major circulating components, accounting for the same 27.45% of the plasma total radioactivity (AUC 0–24h pool), while other circulating metabolites were minor, accounting for less than 10%. Mean C max , AUC 0–∞, T 1/2 and T max values for ensartinib in plasma were 185 ng/mL, 3827 h ng/mL, 18.3 h and 3.25 h, respectively. The total radioactivity in plasma was cleared with terminal half-life of 27.2 h. Treatment with ensartinib was well tolerated, and no serious adverse events were reported. Conclusion It was well tolerated in the six healthy male subjects following a single oral administration of 200 mg/100 μCi dose of ensartinib. Besides unchanged ensartinib, metabolite of M465 was the predominant circulating drug-related component. The drug was primarily eliminated in feces. Clinical trial registration ClinicalTrials.gov NCT03804541.
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