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P-Glycoprotein (ABCB1/MDR1) and BCRP (ABCG2) Limit Brain Accumulation and Cytochrome P450-3A (CYP3A) Restricts Oral Exposure of the RET Inhibitor Selpercatinib (RETEVMO)

Selpercatinib is a targeted, FDA-approved, oral, small-molecule inhibitor for the treatment of rearranged during transfection (RET) proto-oncogene mutation-positive cancer. Using genetically modified mouse models, we investigated the roles of the multidrug efflux transporters ABCB1 and ABCG2, the OA...

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Detalles Bibliográficos
Autores principales:	Wang, Yaogeng, Sparidans, Rolf W., Potters, Sander, Şentürk, Rahime, Lebre, Maria C., Beijnen, Jos H., Schinkel, Alfred H.
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	MDPI 2021
Materias:	Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8617681/ https://www.ncbi.nlm.nih.gov/pubmed/34832869 http://dx.doi.org/10.3390/ph14111087

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