CLINICAL TRIAL article
Front. Pharmacol.
Sec. Drug Metabolism and Transport
Volume 16 - 2025 | doi: 10.3389/fphar.2025.1563556
Evaluation of the pharmacokinetic interactions of montmorillonite powder or loperamide on pyrotinib in healthy volunteers
Provisionally accepted
YIKE WANG1
Dai Li2Tong Zhang1
Sumei Xu2Yanxin Zhang2Kaijing Zhao1Shaorong Li1
Kai Shen1Xiaomin Li2*
Pingsheng Xu2*- 1Jiangsu HengRui Pharmaceuticals, Lianyungang, China
- 2Xiangya Hospital, Central South University, Changsha, Hunan Province, China
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• Pyrotinib is an irreversible dual Human Epidermal growth factor Receptor 2(HER2) and epidermal growth factor receptor(EGFR) tyrosine kinase inhibitor(TKI). Diarrhea is the most common adverse reaction observed in clinical trials of pyrotinib.• Symptomatic management of diarrhea of pyrotinib is usually done by using either montmorillonite powder or loperamide. The population pharmacokinetics found concomitant use of montmorillonite powder could decrease the bioavailability of pyrotinib by 50.3%.• This study investigated the interaction of montmorillonite powder or loperamide on pyrotinib.• Even when montmorillonite powder was administered 2 hours after pyrotinib dosing, it still reduced systemic exposure of pyrotinib by 32.4% in AUC0-∞, potentially through a coating effect on the gastrointestinal mucosa.• Loperamide could increase pyrotinib exposure by 19% in AUC0-∞ potentially through reduced propulsive peristalsis and increased absorption time.• Loperamide is recommended in symptom control in pyrotinib-induced diarrhea.
Keywords: Pyrotinib, Montmorillonite powder, Loperamide, Diarrhea, pharmacokinetics
Received: 22 Jan 2025; Accepted: 16 Apr 2025.
Copyright: © 2025 WANG, Li, Zhang, Xu, Zhang, Zhao, Li, Shen, Li and Xu. 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:
Xiaomin Li, Xiangya Hospital, Central South University, Changsha, 410008, Hunan Province, China
Pingsheng Xu, Xiangya Hospital, Central South University, Changsha, 410008, Hunan Province, China
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.