OATP1A/1B, CYP3A, ABCB1, and ABCG2 limit oral availability of the NTRK inhibitor larotrectinib, while ABCB1 and ABCG2 also restrict its brain accumulation

BACKGROUND AND PURPOSE: Larotrectinib is a FDA‐approved oral small‐molecule inhibitor for treatment of neurotrophic tropomyosin receptor kinase fusion‐positive cancer. We here investigated the functions of the multidrug efflux transporters ABCB1 and ABCG2, the SLCO1A/1B (OATP1A/1B) uptake transporte...

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Detaylı Bibliyografya
Yayımlandı:Br J Pharmacol
Asıl Yazarlar: Wang, Yaogeng, Sparidans, Rolf W., Li, Wenlong, Lebre, Maria C., Beijnen, Jos H., Schinkel, Alfred H.
Materyal Türü: Artigo
Dil:Inglês
Baskı/Yayın Bilgisi: John Wiley and Sons Inc. 2020
Konular:
Research Papers
Online Erişim:https://ncbi.nlm.nih.gov/pmc/articles/PMC7279963/
https://ncbi.nlm.nih.gov/pubmed/32087611
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1111/bph.15034
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