ABCB1 and ABCG2 Control Brain Accumulation and Intestinal Disposition of the Novel ROS1/TRK/ALK Inhibitor Repotrectinib, While OATP1A/1B, ABCG2, and CYP3A Limit Its Oral Availability

Repotrectinib shows high activity against ROS1/TRK/ALK fusion-positive cancers in preclinical studies. We explored the roles of multidrug efflux transporters ABCB1 and ABCG2, the OATP1A/1B uptake transporter(s), and the CYP3A complex in pharmacokinetics and tissue distribution of repotrectinib in ge...

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Main Authors: Wenlong Li (Author), Rolf W. Sparidans (Author), Maria C. Lebre (Author), Jos H. Beijnen (Author), Alfred H. Schinkel (Author)
Format: Book
Published: MDPI AG, 2021-10-01T00:00:00Z.
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3rd Floor Main Library

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Call Number: A1234.567
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