Effect of itraconazole on pharmacokinetics of ZX-7101A tablets in healthy Chinese subjects

作者：Junzhen Wu, Wang Yin, Wei Liu, Jinjie He, Jufang Wu, Jicheng Yu, Xiaojie Wu, Jianguang Su, Mei Liu, Yilin Li, Jing Zhang · 发表于：Frontiers in Pharmacology · 年份：2025 · DOI：10.3389/fphar.2025.1722747 · 被引用次数：1 · 研究领域：Pharmacogenetics and Drug Metabolism、Phytochemistry Medicinal Plant Applications、Antifungal resistance and susceptibility

Aims A single-center, open label trial was conducted to evaluate the effects of itraconazole on the pharmacokinetics of ZX-7101A tablets in healthy Chinese adults. Methods Subjects took a single dose of 40 mg ZX-7101A tablets on Day 1 on Day 31following once-daily itraconazole administration (200 mg, Days 26–50). The concentrations of ZX-7101A and ZX-7101 in plasma samples were determined by liquid chromatography–tandem mass spectrometry. Pharmacokinetic (PK) parameters of ZX-7101A and ZX-7101 were calculated, and the effects of itraconazole on the PK of ZX-7101 were evaluated. Results The median T max of ZX-7101 was 4 h. In stage 1, the mean (±SD) C max , AUC 0-t , AUC 0-inf , and t 1/2 of ZX-7101 were 90.86 ± 44.48 ng/mL, 6313.72 ± 1095.17 h*ng/mL, 6827.31 ± 1163.30 h*ng/mL, and 126.40 ± 28.88 h, respectively. In stage 2, the corresponding values were 117.63 ± 29.95 ng/mL, 9706.83 ± 1062.56 h*ng/mL, 10785.99 ± 1389.08 h*ng/mL, and 148.62 ± 28.72 h. Itraconazole increased ZX-7101 C max , AUC 0-t , and AUC 0-inf by 29.5%, 53.7%, and 58.0%, respectively, and prolonged t 1/2 of ZX-7101 by 17.6%. Conclusion The ZX-7101 exposure after coadministration with itraconazole is lower than the exposure after a single dose of 80 mg ZX-7101A tablets. It is therefore not necessary to adjust the dose of ZX-7101A 40 mg when coadministered with itraconazole. Trial registration http://www.chinadrugtrials.org.cn , identifier: CTR20231556.