https://www.selleckchem.com/pr....oducts/epacadostat-i
Pralsetinib is an FDA-approved oral small-molecule inhibitor for treatment of rearranged during transfection (RET) proto-oncogene fusion-positive non-small cell lung cancer. We investigated how the efflux transporters ABCB1 and ABCG2, the SLCO1A/1B uptake transporters and the drug-metabolizing enzyme CYP3A influence pralsetinib pharmacokinetics. In vitro, transepithelial pralsetinib transport was assessed. In vivo, pralsetinib (10mg/kg) was administered orally to relevant genetically modified mouse models. Pralsetinib con