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ABCB1 and ABCG2, but not CYP3A4 limit oral availability and brain accumulation of the RET inhibitor pralsetinib.
Wang, Yaogeng; Sparidans, Rolf W; Potters, Sander; Lebre, Maria C; Beijnen, Jos H; Schinkel, Alfred H.
Affiliation
  • Wang Y; The Netherlands Cancer Institute, Division of Pharmacology, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands.
  • Sparidans RW; Utrecht University, Faculty of Science, Department of Pharmaceutical Sciences, Division of Pharmacology, Universiteitsweg 99, 3584 CG Utrecht, The Netherlands.
  • Potters S; Leiden university, Faculty of Science, Leiden Academic Centre for Drug Research (LACDR), Einsteinweg 55, 2300 RA Leiden, The Netherlands.
  • Lebre MC; The Netherlands Cancer Institute, Division of Pharmacology, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands.
  • Beijnen JH; The Netherlands Cancer Institute, Division of Pharmacology, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands; Utrecht University, Faculty of Science, Department of Pharmaceutical Sciences, Division of Pharmacology, Universiteitsweg 99, 3584 CG Utrecht, The Netherlands; The Netherlands Cancer Inst
  • Schinkel AH; The Netherlands Cancer Institute, Division of Pharmacology, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands. Electronic address: a.schinkel@nki.nl.
Pharmacol Res ; 172: 105850, 2021 10.
Article in En | MEDLINE | ID: mdl-34450308
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Full text: 1 Database: MEDLINE Main subject: Pyrazoles / Pyridines / Pyrimidines / Organic Anion Transporters / Protein Kinase Inhibitors / Proto-Oncogene Proteins c-ret / Antineoplastic Agents Limits: Animals Language: En Year: 2021 Type: Article
Fulltext
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Full text: 1 Database: MEDLINE Main subject: Pyrazoles / Pyridines / Pyrimidines / Organic Anion Transporters / Protein Kinase Inhibitors / Proto-Oncogene Proteins c-ret / Antineoplastic Agents Limits: Animals Language: En Year: 2021 Type: Article