Stephanie van Hoppe

Preface 7
Chapter 1 Introduction 9
Chapter 2 Breast cancer resistance protein (BCRP/ABCG2) and P-glycoprotein (P-gp/ABCB1) transport afatinib and restrict its oral availability and brain accumulation 21
Chapter 3 Brain accumulation of osimertinib and its active metabolite AZ5104 is restricted by ABCB1 (P-glycoprotein) and ABCG2 (Breast Cancer Resistance Protein) 43
Chapter 4 P-glycoprotein (MDR1/ABCB1) restricts brain penetration of the Bruton’s tyrosine kinase inhibitor ibrutinib while Cytochrome P450-3A (CYP3A) limits its oral bioavailability 69
Chapter 5 Brain accumulation of ponatinib and its active metabolite N-desmethyl ponatinib is limited by P-glycoprotein (PGP/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) 99
Chapter 6 The impact of Organic Anion-Transporting Polypeptides (OATPs) on disposition and toxicity of antitumor drugs; insights from knockout and humanized mice 125
Chapter 7 Conclusions and future perspectives 167
Chapter 8 Summary 173
Nederlandse samenvatting 181
Résumé en français 183
Curriculum vitae 185
List of publications 186
Acknowledgements 188