Breast cancer resistance protein (BCRP/ABCG2) and P-glycoprotein (P-gp/ABCB1) transport afatinib and restrict its oral availability and brain accumulation
作者： Stéphanie van Hoppe , Rolf W. Sparidans , Els Wagenaar , Jos H. Beijnen , Alfred H. Schinkel
DOI: 10.1016/J.PHRS.2017.01.035
关键词:
摘要: Afatinib is a highly selective, irreversible inhibitor of EGFR and HER-2. It is orally administered for the treatment of patients with EGFR mutation-positive types of metastatic NSCLC. We …
narcis.nl参考文章(42)
Seng Chuan Tang, Anita Kort, Ka Lei Cheung, Hilde Rosing, Tatsuki Fukami, Selvi Durmus, Els Wagenaar, Jeroen J. M. A. Hendrikx, Miki Nakajima, Bart J. M. van Vlijmen, Jos H. Beijnen, Alfred H. Schinkel, P-glycoprotein, CYP3A, and Plasma Carboxylesterase Determine Brain Disposition and Oral Availability of the Novel Taxane Cabazitaxel (Jevtana) in Mice. Molecular Pharmaceutics. ,vol. 12, pp. 3714- 3723 ,(2015) , 10.1021/ACS.MOLPHARMACEUT.5B00470
Anita Kort, Rolf W. Sparidans, Els Wagenaar, Jos H. Beijnen, Alfred H. Schinkel, Brain accumulation of the EML4-ALK inhibitor ceritinib is restricted by P-glycoprotein (P-GP/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) Pharmacological Research. ,vol. 102, pp. 200- 207 ,(2015) , 10.1016/J.PHRS.2015.09.003
Alessio Di Luca, Michael Henry, Paula Meleady, Robert O’Connor, Label-free LC-MS analysis of HER2+ breast cancer cell line response to HER2 inhibitor treatment. DARU. ,vol. 23, pp. 40- 40 ,(2015) , 10.1186/S40199-015-0120-Y
Joseph W. Polli, Katie L. Olson, John P. Chism, Lisa St. John-Williams, Russell L. Yeager, Sesha M. Woodard, Vicky Otto, Stephen Castellino, Victoria E. Demby, An Unexpected Synergist Role of P-Glycoprotein and Breast Cancer Resistance Protein on the Central Nervous System Penetration of the Tyrosine Kinase Inhibitor Lapatinib (N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine; GW572016) Drug Metabolism and Disposition. ,vol. 37, pp. 439- 442 ,(2009) , 10.1124/DMD.108.024646
Yosef Yarden, Mark X. Sliwkowski, Untangling the ErbB signalling network Nature Reviews Molecular Cell Biology. ,vol. 2, pp. 127- 137 ,(2001) , 10.1038/35052073
Nancy E. Hynes, Heidi A. Lane, ERBB receptors and cancer: the complexity of targeted inhibitors. Nature Reviews Cancer. ,vol. 5, pp. 341- 354 ,(2005) , 10.1038/NRC1609
Seng Chuan Tang, Jurjen S. Lagas, Nienke A.G. Lankheet, Birk Poller, Michel J. Hillebrand, Hilde Rosing, Jos H. Beijnen, Alfred H. Schinkel, Brain accumulation of sunitinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by oral elacridar and sunitinib coadministration International Journal of Cancer. ,vol. 130, pp. 223- 233 ,(2012) , 10.1002/IJC.26000
Roos L. Oostendorp, Tessa Buckle, Jos H. Beijnen, Olaf van Tellingen, Jan H. M. Schellens, The effect of P-gp (Mdr1a/1b), BCRP (Bcrp1) and P-gp/BCRP inhibitors on the in vivo absorption, distribution, metabolism and excretion of imatinib. Investigational New Drugs. ,vol. 27, pp. 31- 40 ,(2009) , 10.1007/S10637-008-9138-Z
J. Cory Kalvass, Gary M. Pollack, Kinetic considerations for the quantitative assessment of efflux activity and inhibition: implications for understanding and predicting the effects of efflux inhibition. Pharmaceutical Research. ,vol. 24, pp. 265- 276 ,(2007) , 10.1007/S11095-006-9135-X
A H Schinkel, E Wagenaar, C A Mol, L van Deemter, P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs. Journal of Clinical Investigation. ,vol. 97, pp. 2517- 2524 ,(1996) , 10.1172/JCI118699