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P-Glycoprotein (MDR1/ABCB1) Restricts Brain Accumulation of the Novel EGFR Inhibitor EAI045 and Oral Elacridar Coadministration Enhances Its Brain Accumulation and Oral Exposure

EAI045 is a fourth-generation allosteric tyrosine kinase inhibitor (TKI) of the epidermal growth factor receptor (EGFR). It targets T790M and C797S EGFR mutants in the treatment of non-small cell lung cancer (NSCLC). EAI045 and cetuximab combined induce tumor regression in mouse models of EGFR-mutan...

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Detalles Bibliográficos
Autores principales: Wang, Jing, Susam, M. Merve, Gan, Changpei, Sparidans, Rolf W., Lebre, Maria C., Beijnen, Jos H., Schinkel, Alfred H.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9505538/
https://www.ncbi.nlm.nih.gov/pubmed/36145346
http://dx.doi.org/10.3390/ph15091124