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Review

Lapatinib-Based Radioagents for Application in Nuclear Medicine

by
Przemysław Koźmiński
* and
Ewa Gniazdowska
*
Centre of Radiochemistry and Nuclear Chemistry, Institute of Nuclear Chemistry and Technology, 03-195 Warsaw, Poland
*
Authors to whom correspondence should be addressed.
Appl. Sci. 2025, 15(20), 10964; https://doi.org/10.3390/app152010964 (registering DOI)
Submission received: 9 September 2025 / Revised: 10 October 2025 / Accepted: 11 October 2025 / Published: 12 October 2025

Abstract

Lapatinib is an approved therapeutic agent for the treatment of HER2-positive breast cancer. It has a high affinity for the non-receptor cytoplasmic tyrosine kinases of the EGFR and HER2 receptors. It is a type II inhibitor, with Kiapp values of 3 nM and 13 nM, respectively. The dissociation rate of the lapatinib–receptor complex is notably slow compared with many other kinase inhibitors. Although the literature contains numerous reports on radiolabelled ligands for HER-family receptors, studies on radiolabelled tyrosine kinase inhibitors are far fewer, and only few focus specifically on radiolabelled lapatinib. The aim of this review is to compile and discuss the chemical and biological data on lapatinib-based radiopharmaceuticals with potential applications in the diagnosis and treatment of HER2-positive tumours.
Keywords: receptors (HER2, EGFR, IGF-1); tyrosine kinase; radionuclides; radiopharmaceuticals receptors (HER2, EGFR, IGF-1); tyrosine kinase; radionuclides; radiopharmaceuticals

Share and Cite

MDPI and ACS Style

Koźmiński, P.; Gniazdowska, E. Lapatinib-Based Radioagents for Application in Nuclear Medicine. Appl. Sci. 2025, 15, 10964. https://doi.org/10.3390/app152010964

AMA Style

Koźmiński P, Gniazdowska E. Lapatinib-Based Radioagents for Application in Nuclear Medicine. Applied Sciences. 2025; 15(20):10964. https://doi.org/10.3390/app152010964

Chicago/Turabian Style

Koźmiński, Przemysław, and Ewa Gniazdowska. 2025. "Lapatinib-Based Radioagents for Application in Nuclear Medicine" Applied Sciences 15, no. 20: 10964. https://doi.org/10.3390/app152010964

APA Style

Koźmiński, P., & Gniazdowska, E. (2025). Lapatinib-Based Radioagents for Application in Nuclear Medicine. Applied Sciences, 15(20), 10964. https://doi.org/10.3390/app152010964

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