ABCB1 and ABCG2, but not CYP3A4 limit oral availability and brain accumulation of the RET inhibitor pralsetinib
Yaogeng Wang, Rolf W. Sparidans, Sander Potters, Maria C. Lebre, Jos H. Beijnen, Alfred H. Schinkel
Topics & Concepts
PharmacokineticsAbcg2PharmacologyIn vivoCYP3A4ChemistryOral administrationEffluxBioavailabilityTransporterATP-binding cassette transporterBiologyMetabolismBiochemistryCytochrome P450GeneBiotechnologyDrug Transport and Resistance MechanismsLung Cancer Treatments and MutationsHedgehog Signaling Pathway Studies