Year: 2025
Type: article
Abstract: Lapatinib is an approved therapy for 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 reversible 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 tumors.
Source: Applied Sciences
DOI: 10.3390/app152010964
Authors: Przemysław Koźmiński, Ewa Gniazdowska
Institution: Instytut Chemii i Techniki Jądrowej
Language: English
Subfield: Radiology, Nuclear Medicine and Imaging
Field: Medicine
Domain: Health Sciences
Open Access status: gold
Estimated APC paid: $2,896
Award: G2126062883
OpenAlex ID: W4415117312