Drug intelligence / Profile preview

lapatinib + samarium-153

Development stage
Preclinical
Lead developer
Dalat Nuclear Research Institute
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

The experimental radiopharmaceutical combination of lapatinib and samarium-153 (specifically formulated as Fe3O4@lapatinib-153Sm nanoparticles) is being developed by the Dalat Nuclear Research Institute and Duy Tan University for the treatment of HER2-positive breast cancer. The formulation consists of superparamagnetic iron oxide (Fe3O4) nanoparticles co-precipitated with the dual EGFR/HER2 tyrosine kinase inhibitor lapatinib and radiolabeled with the beta- and gamma-emitting radioisotope samarium-153 (153Sm). Lapatinib provides targeted delivery to HER2-overexpressing cancer cells and exerts therapeutic kinase inhibition, while the Fe3O4 core offers magnetic targeting and MRI contrast enhancement. The samarium-153 component delivers localized beta-radiation for targeted tumor cell destruction and emits gamma radiation suitable for SPECT imaging and dosimetry. Preclinical studies in murine models have demonstrated high radiolabeling efficiency, favorable biodistribution with significant tumor accumulation, and manageable toxicity.

Other names
153Sm-labeled Fe3O4@lapatinib nanoparticlesFe3O4-coated lapatinib-labeled 153Sm nanoparticlesFe-3O4-coated lapatinib-labeled 153Sm nanoparticlesFe 3O4-coated lapatinib-labeled 153Sm nanoparticlesFe3O4@lapatinib-153Smsamarium-153-labeled Fe3O4@lapatinib nanoparticles
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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