REVIEW article
Oncol. Rev.
Sec. Oncology Reviews: Reviews
Volume 19 - 2025 | doi: 10.3389/or.2025.1612249
Tyrosine-Kinase Inhibitors for Lung or Breast Cancer and Drug-Drug-interactions: a clinical guide
Provisionally accepted- 1Department of Experimental Medicine, Faculty of Medicine and Dentistry, Sapienza University of Rome, Rome, Lazio, Italy
- 2Umberto 1 Hospital, Rome, Sicily, Italy
- 3Sapienza University of Rome, Rome, Lazio, Italy
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Introduction: In the last two decades, Tyrosine-kinase inhibitors (TKIs) have dramatically changed prognosis among Lung and Breast Cancers, with a significant benefit in metastatic and, more recently, in the adjuvant setting in selected groups of patients. Despite their favorable oncological action, TKIs are at high risk for Drug-Drug-Interactions (DDIs) due to their pharmacokinetic (PK) depending both on pH-dependent absorption and on liver metabolism. However, the DDIs are frequently related to “potential DDI” (pDDI) and their relevance in clinical practice often underestimated and there is a lack of practical guide for clinicians. Methods and Materials: We conducted a narrative review restricted to the last twenty years, to adults (aged 18 years or older) with lung or breast cancers treated with TKIs and clinical data of potential DDIs and with reported toxicities or outcome. Results: We summarized the pharmacokinetic profile and the clinical evidence of eleven TKIs used for Lung or Breast Cancers. Moreover, we provided an easy-to-use guide to help physicians in clinical practice with recommended dose adjustment or cautions required for preventing severe adverse events or possible change in TKIs availability in presence of other interfering drugs. Conclusions: The level of evidence for DDIs during TKI treatment is low because most available data are from phase I studies in healthy volunteers and few phase II studies in cancer patients. However, since the occurrence of DDIs could be clinically significant as well as a prompt drug reconciliation process useful to prevent it, further, prospective, large sample size clinical trials should be carried out.
Keywords: Tyrosine-kinase inhibitors (TKIs), lung cancer, NSCLC - lung adenocarcinoma - EGFR - ALK - BRAF - KRAS - RET - MET - PD-L1 - ROS1, breast cancer, Drug - drug interactions, HER2 breast cancer +
Received: 15 Apr 2025; Accepted: 04 Aug 2025.
Copyright: © 2025 Santamaria, Roberto, Maltese, Nicolella, Torchia, Buccilli, Di Civita, Giancontieri, Marinelli, Cirillo, Bianco, Verrico, Botticelli and Santini. 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: Fiorenza Santamaria, Department of Experimental Medicine, Faculty of Medicine and Dentistry, Sapienza University of Rome, Rome, 00185, Lazio, Italy
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