P-glycoprotein and breast cancer resistance protein restrict brigatinib brain accumulation and toxicity, and, alongside CYP3A, limit its oral availability

Article ID	Journal	Published Year	Pages	File Type
11025705	Pharmacological Research	2018	39 Pages	PDF

Keywords

ABC TKI P-gp BTB MDCK area under plasma concentration-time curve Bcrp tmax Brigatinib CyP Cmax AUC LC–MS/MS P-glycoprotein ALK standard deviation Human analysis of variance ANOVA Oral availability CNS BBB NSCLC Non-small cell lung cancer Cytochrome P450 central nervous system Brain concentration Anaplastic lymphoma kinase Blood-testis barrier Blood-brain barrier Tyrosine kinase inhibitor Mouse breast cancer resistance protein liquid chromatography coupled with tandem mass spectrometry Madin-Darby canine kidney ATP-binding cassette

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P-glycoprotein and breast cancer resistance protein restrict brigatinib brain accumulation and toxicity, and, alongside CYP3A, limit its oral availability

Authors

Wenlong Li, Rolf W. Sparidans, Yaogeng Wang, Maria C. Lebre, Jos H. Beijnen, Alfred H. Schinkel,