ArticleScientific reports2018
Distribution analysis of epertinib in brain metastasis of HER2-positive breast cancer by imaging mass spectrometry and prospect for antitumor activity.
Article in Scientific reports, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 37 citations in OpenAlex.
- A phase I/II study of epertinib plus trastuzumab with or without chemotherapy in patients with HER2-positive metastatic breast cancer.Breast cancer research : BCR · 2019Trial
- Spatial Distribution of Brain PET Tracers by MALDI Imaging.Journal of the American Society for Mass Spectrometry · 2025Article
- Molecular Targeting of the Human Epidermal Growth Factor Receptor-2 (HER2) Genes across Various Cancers.International journal of molecular sciences · 2024Review
- Unlocking New Avenues in Breast Cancer Treatment: The Synergy of Kinase Inhibitors and Immunotherapy.Cancers · 2023Review
- Detection of Distinct Distributions of Acetaminophen and Acetaminophen-Cysteine in Kidneys up to 10 μm Resolution and Identification of a Novel Acetaminophen Metabolite Using an AP-MALDI Imaging Mass Microscope.Journal of the American Society for Mass Spectrometry · 2023Article
- Dissecting the brain with spatially resolved multi-omics.Journal of pharmaceutical analysis · 2023Review
- Review
- Imaging Technologies for Cerebral Pharmacokinetic Studies: Progress and Perspectives.Biomedicines · 2022Review
- Spatial analysis of drug absorption, distribution, metabolism, and toxicology using mass spectrometry imaging.Biochemical pharmacology · 2022Review
- Analytical Performance Evaluation of New DESI Enhancements for Targeted Drug Quantification in Tissue Sections.Pharmaceuticals (Basel, Switzerland) · 2022Article
- HER2-positive breast cancer brain metastasis: A new and exciting landscape.Cancer reports (Hoboken, N.J.) · 2022Review
- A common goal to CARE: Cancer Advocates, Researchers, and Clinicians Explore current treatments and clinical trials for breast cancer brain metastases.NPJ breast cancer · 2021Review
- [Mass spectrometry imaging technology and its application in breast cancer research].Se pu = Chinese journal of chromatography · 2021Review
- The In Vivo Selection Method in Breast Cancer Metastasis.International journal of molecular sciences · 2021Review
- Modelling the structural and reactivity landscapes of tucatinib with special reference to its wavefunction-dependent properties and screening for potential antiviral activity.Journal of molecular modeling · 2020Article
- Considerations for MALDI-Based Quantitative Mass Spectrometry Imaging Studies.Journal of proteome research · 2020Article
- Quantitative determination of niraparib and olaparib tumor distribution by mass spectrometry imaging.International journal of biological sciences · 2020Article
- Tissue Imaging by Mass Spectrometry: A Practical Guide for the Medicinal Chemist.ACS medicinal chemistry letters · 2019Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Epertinib (S-222611) is a potent, reversible, and selective tyrosine kinase inhibitor of epidermal growth factor receptor (EGFR), human EGFR2 (HER2), and human EGFR4. We developed experimental brain metastasis models by intraventricular injection (intraventricular injection mouse model; IVM) of HER2-positive breast cancer (MDA-MB-361-luc-BR2/BR3) or T790M-EGFR-positive lung cancer (NCI-H1975-luc) cells. After a single oral administration, epertinib and lapatinib concentrations in brain metastatic regions were analyzed by quantitative imaging mass spectrometry. In the NCI-H1975 lung cancer IVM, the concentration of epertinib in brain metastasis was comparable to that of lapatinib. However, in the MDA-MB-361 breast cancer IVM, the concentration of epertinib in brain metastasis was >10 times higher than that of lapatinib. Furthermore, the epertinib tumor-to-normal brain ratio was ~4 times higher than that of lapatinib. Blood-tumor barrier (BTB) permeability was assessed in each brain metastatic region. In the lung cancer model, fluorescently labeled dextran was more highly detected in brain metastatic regions than in brain parenchyma. However, in breast cancer models, dextran fluorescence intensity in brain metastatic regions and brain parenchyma were comparable, suggesting that the BTB remained largely intact. Epertinib would be promised as a therapeutic agent for HER2-positive breast cancer with brain metastasis.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.