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

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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Bibliographic Details
Main Authors: Yaogeng Wang, Rolf W. Sparidans, Sander Potters, Rahime Şentürk, Maria C. Lebre, Jos H. Beijnen, Alfred H. Schinkel
Format: Article
Language:English
Published: MDPI AG 2021-10-01
Series:Pharmaceuticals
Subjects:
selpercatinib
cytochrome P450-3A
oral exposure
rearranged during transfection (RET) receptor kinase
Slco1a/1b
p-glycoprotein/ABCB1
Online Access:https://www.mdpi.com/1424-8247/14/11/1087

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https://www.mdpi.com/1424-8247/14/11/1087

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