CLINICAL TRIAL article
Front. Pharmacol.
Sec. Drug Metabolism and Transport
Volume 16 - 2025 | doi: 10.3389/fphar.2025.1636504
This article is part of the Research TopicNew Drugs and Future Challenges in Drug Metabolism and TransportView all 26 articles
A Phase I Study of HEC73543, an oral FLT3 inhibitor: the Effect of Food on Pharmacokinetics after Oral Dosing in Healthy Chinese Volunteers
Provisionally accepted
- 1The First Hospital of Jilin University Department of Phase I Clinical Trial Unit, Changchun, China
- 2Sunshine Lake Pharma Company, Ltd., Dongguan, China
- 3State Key Laboratory of Anti-Infective Drug Discovery and Development, Sunshine Lake Pharma Company, Ltd., Dongguan, China
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Objective: This study evaluated the effect of food on the pharmacokinetics (PK) and safety of HEC73543. Methods: This randomized, open-label, single-dose, phase I parallel trial included 40 healthy subjects randomized (1:1) to either high-fat or fasted groups. Participants received a single oral dose of 40mg HEC73543. Blood samples were collected and detected using a validated liquid chromatography tandem mass spectrometry method. PK parameters were calculated using non-compartmental methods. Safety was monitored throughout the study. Results: For the HEC73543, the fed-to-fasted ratios were: area under the curve from time 0 to time t (AUC0–t), 219.42% (90% confidence interval [CI]: 173.76, 277.08%); AUC from zero to infinity (AUC0–∞), 255.22% (90% CI: 198.10, 328.80%); and maximum concentration (Cmax), 221.31% (90%CI: 190.57, 257.00%). Similarly, for the metabolite M3, the fed-to-fasted ratios were: AUC0–t, 190.86% (90%CI: 153.26%, 237.68%); AUC0–∞, 190.29% (90% CI: 151.77%, 238.59%); and Cmax, 177.48% (90% CI: 137.80%, 228.58%). Median Tmax were comparable between the two groups. The most frequently Treatment-Related Adverse Events (TRAEs) were elevated blood triglycerides, oral ulceration, hyperuricemia, diarrhea, thoracalgia. Most TRAEs were Grade 1 or 2. Conclusion: High-fat food intake enhanced bioavailability and increases the systemic exposure levels of HEC73543 and its metabolite M3. Clinical trial registration: NCT05454098 (http://www.clinicaltrials.gov/).
Keywords: AML, HEC73543, FLT3 inhibitor, Food effect, pharmacokinetics
Received: 28 May 2025; Accepted: 22 Sep 2025.
Copyright: © 2025 Wang, Wu, Li, Jiang, Liu, Zhang, Deng and Ding. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
* Correspondence:
Li Deng, dengli@hec.cn
Yanhua Ding, dingyanh@jlu.edu.cn
Disclaimer: All claims expressed in this article are solely those of the authors and do not necessarily represent those of their affiliated organizations, or those of the publisher, the editors and the reviewers. Any product that may be evaluated in this article or claim that may be made by its manufacturer is not guaranteed or endorsed by the publisher.