Stephanie van Hoppe

88 Chapter 4 R E F E R E N C E S 1. Schinkel, A.H., et al., P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs. J Clin Invest, 1996. 97(11): p. 2517-24. 2. Vlaming, M.L., J.S. Lagas, and A.H. Schinkel, Physiological and pharmacological roles of ABCG2 (BCRP): recent findings in Abcg2 knockout mice. Adv Drug Deliv Rev, 2009. 61(1): p. 14-25. 3. Yabuki, N., et al., Gene amplification and expression in lung cancer cells with acquired paclitaxel resistance. Cancer Genet Cytogenet, 2007. 173(1): p. 1-9. 4. van Hoppe, S., et al., Breast cancer resistance protein (BCRP/ABCG2) and P-glycoprotein (P-gp/ABCB1) transport afatinib and restrict its oral availability and brain accumulation. Pharmacol Res, 2017. 120: p. 43- 50. 5. Stuurman, F.E., et al., Oral anticancer drugs: mechanisms of low bioavailability and strategies for improvement. Clin Pharmacokinet, 2013. 52(6): p. 399-414. 6. Center for Drug valuation and Research of the U.S., Department of Health and Human Services Food and Drug Administration. . 2017; Available from: https://www.accessdata.fda.gov/drugsatfda_docs/ label/2017/205552s017lbl.pdf. 7. Masso-Valles, D., et al., Ibrutinib exerts potent antifibrotic and antitumor activities in mouse models of pancreatic adenocarcinoma. Cancer Res, 2015. 75(8): p. 1675-81. 8. Rauf, F., et al., Ibrutinib inhibition of ERBB4 reduces cell growth in a WNT5A-dependent manner. Oncogene, 2018. 9. Sagiv-Barfi, I., et al., Therapeutic antitumor immunity by checkpoint blockade is enhanced by ibrutinib, an inhibitor of both BTK and ITK. Proc Natl Acad Sci U S A, 2015. 112(9): p. E966-72. 10. Berglof, A., et al., Targets for Ibrutinib Beyond B Cell Malignancies. Scand J Immunol, 2015. 82(3): p. 208-17. 11. Busygina, K., et al., Oral Bruton tyrosine kinase inhibitors selectively block atherosclerotic plaque-triggered thrombus formation. Blood, 2018. 12. Honigberg, L.A., et al., The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious inmodels of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci U S A, 2010. 107(29): p. 13075-80. 13. Wang, X., et al., Bruton’s Tyrosine Kinase Inhibitors Prevent Therapeutic Escape in Breast Cancer Cells. Mol Cancer Ther, 2016. 15(9): p. 2198-208. 14. Zhang, H., et al., The BTK Inhibitor Ibrutinib (PCI-32765) Overcomes Paclitaxel Resistance in ABCB1- and ABCC10-Overexpressing Cells and Tumors. Mol Cancer Ther, 2017. 16(6): p. 1021-1030. 15. Scheers, E., et al., Absorption, metabolism, and excretion of oral (1)(4)C radiolabeled ibrutinib: an open-label, phase I, single-dose study in healthy men. Drug Metab Dispos, 2015. 43(2): p. 289-97. 16. Center for Drug valuation and Research of the U.S., Department of Health and Human Services Food and Drug Administration, 203469Orig1s000 . 2012; Available from: http://www.accessdata.fda.gov/drugsatfda_ docs/nda/2012/203469Orig1s000ClinPharmR.pdf. 17. Novartis Pharmaceuticals Corporation, Gleevec [prescribing information] 2004; Available from: https:// www.pharma.us.novartis.com/sites/www.pharma.us.novartis.com/files/gleevec_tabs.pdf. 18. Novartis Pharmaceuticals, Tasigna [package insert] . 2014; Available from: https://www.pharma.us.novartis . com/product/pi/pdf/tasigna.pdf. 19. Li, X., et al., Characterization of dasatinib and its structural analogs as CYP3A4mechanism-based inactivators and the proposed bioactivation pathways. Drug Metab Dispos, 2009. 37(6): p. 1242-50. 20. Abbas, R., et al., Effect of ketoconazole on the pharmacokinetics of oral bosutinib in healthy subjects. J Clin Pharmacol, 2011. 51(12): p. 1721-7. 21. Rood, J.J., et al., Liquid chromatography-tandem mass spectrometric assay for the simultaneous determination of the irreversible BTK inhibitor ibrutinib and its dihydrodiol-metabolite in plasma and its application in mouse pharmacokinetic studies. J Pharm Biomed Anal, 2016. 118: p. 123-31. 22. Durmus, S., et al., Oral availability and brain penetration of the B-RAFV600E inhibitor vemurafenib can be enhanced by the P-GLYCOprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar. Mol Pharm, 2012. 9(11): p. 3236-45.

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