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[11C] lapatinib

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

[11C] lapatinib is a radiolabeled form of the small molecule tyrosine kinase inhibitor lapatinib, in which the drug is tagged with the radioactive isotope carbon-11 for use in positron emission tomography (PET) imaging. Lapatinib itself is an orally active, reversible inhibitor of both epidermal growth factor receptor (EGFR/ERBB1/HER1) and human epidermal growth factor receptor 2 (HER2/ERBB2), blocking their intracellular tyrosine kinase domains and thereby inhibiting downstream signaling pathways that promote tumor cell proliferation and survival[1][6][8]. The [11C]-labeled version enables non-invasive imaging to study drug distribution, particularly blood-brain barrier penetration and uptake into brain metastases in patients with HER2-positive breast cancer[6][8][10]. It has been used primarily as a research tool to assess pharmacokinetics and tissue distribution rather than as a therapeutic agent.

Other names
carbon-11 radiolabeled lapatinibcarbon11 radiolabeled lapatinibcarbon 11 radiolabeled lapatinib[(11)C]lapatinib
02

Targets

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

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