Stephanie van Hoppe

60 Chapter 3 CON C LU S I ON Our study shows that ABCB1 andABCG2donot restrict theoral availability of osimertinib, but that they do markedly restrict the brain disposition of both osimertinib and AZ5104. These results suggest that coadministration of ABCB1 and ABCG2 inhibitors may be an option to enhance osimertinib exposure in patients, especially in the brain. This could provide a better option to treat NSCLC and its metastases located in part or in whole behind a functional blood-brain barrier.