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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Detalles Bibliográficos
Autores principales: Li, Wenlong, Sparidans, Rolf W., 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/PMC8619046/
https://www.ncbi.nlm.nih.gov/pubmed/34834176
http://dx.doi.org/10.3390/pharmaceutics13111761

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8619046/
https://www.ncbi.nlm.nih.gov/pubmed/34834176
http://dx.doi.org/10.3390/pharmaceutics13111761

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