ABCG2-and ABCB1 Inhibition Using Supratherapeutic Doses of Erlotinib: Clinical Implications in the Treatment of Central Nervous System Metastases
EA van de Stadt, M Yaqub, I Bahce… - Journal of Nuclear …, 2020 - Soc Nuclear Med
TO THE EDITOR: We read with great interest the article by Bauer et al. titled ''A Proof-of-
Concept Study to Inhibit ABCG2-and ABCB1-Mediated Efflux Transport at the Human Blood …
Concept Study to Inhibit ABCG2-and ABCB1-Mediated Efflux Transport at the Human Blood …
Strategies to inhibit ABCB1-and ABCG2-mediated efflux transport of erlotinib at the blood–brain barrier: a PET study on nonhuman primates
N Tournier, S Goutal, S Auvity, A Traxl… - Journal of Nuclear …, 2017 - Soc Nuclear Med
The tyrosine kinase inhibitor erlotinib poorly penetrates the blood–brain barrier (BBB)
because of efflux transport by P-glycoprotein (ABCB1) and breast cancer resistance protein …
because of efflux transport by P-glycoprotein (ABCB1) and breast cancer resistance protein …
A proof-of-concept study to inhibit ABCG2-and ABCB1-mediated efflux transport at the human blood–brain barrier
M Bauer, R Karch, B Wulkersdorfer… - Journal of Nuclear …, 2019 - Soc Nuclear Med
The adenosine triphosphate-binding cassette transporters P-glycoprotein (ABCB1) and
breast cancer resistance protein (ABCG2) are 2 efflux transporters at the blood–brain barrier …
breast cancer resistance protein (ABCG2) are 2 efflux transporters at the blood–brain barrier …
[PDF][PDF] Pharmacokinetic imaging with radiolabeled molecularly targeted anticancer drugs
We would like to thank van de Stadt and colleagues for their positive and encouraging
comments regarding our study recently published in JNM (1). The central nervous system …
comments regarding our study recently published in JNM (1). The central nervous system …
Molecular imaging of ABCB1 and ABCG2 inhibition at the human blood–brain barrier using Elacridar and 11C-Erlotinib PET
RB Verheijen, M Yaqub, E Sawicki… - Journal of Nuclear …, 2018 - Soc Nuclear Med
Transporters such as ABCB1 and ABCG2 limit the exposure of several anticancer drugs to
the brain, leading to suboptimal treatment in the central nervous system. The purpose of this …
the brain, leading to suboptimal treatment in the central nervous system. The purpose of this …
Role of ATP-binding cassette and solute carrier transporters in erlotinib CNS penetration and intracellular accumulation
MA Elmeliegy, AM Carcaboso, M Tagen, F Bai… - Clinical Cancer …, 2011 - AACR
Purpose: To study the role of drug transporters in central nervous system (CNS) penetration
and cellular accumulation of erlotinib and its metabolite, OSI-420. Experimental Design …
and cellular accumulation of erlotinib and its metabolite, OSI-420. Experimental Design …
Inhibition of ABCB1 and ABCG2 at the Mouse Blood–Brain Barrier with Marketed Drugs To Improve Brain Delivery of the Model ABCB1/ABCG2 Substrate [11C] …
A Traxl, S Mairinger, T Filip, M Sauberer… - Molecular …, 2019 - ACS Publications
P-Glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) are two efflux
transporters at the blood–brain barrier (BBB), which effectively restrict brain distribution of …
transporters at the blood–brain barrier (BBB), which effectively restrict brain distribution of …
Breast cancer resistance protein and P-glycoprotein influence in vivo disposition of 11C-erlotinib
A Traxl, T Wanek, S Mairinger, J Stanek… - Journal of Nuclear …, 2015 - Soc Nuclear Med
11C-erlotinib is a PET tracer to distinguish responders from nonresponders to epidermal
growth factor receptor–targeted tyrosine kinase inhibitors and may also be of interest to …
growth factor receptor–targeted tyrosine kinase inhibitors and may also be of interest to …
The impact of the ABC transporters P-gp and BCRP on the oral bioavailability and brain penetration of erlotinib using drug transporter knockout mouse models.
O van Tellingen, S Marchetti, N de Vries, J Zhao… - Cancer Research, 2007 - AACR
Abstract LB-373 The ABC transporters P-glycoprotein (Pgp, MDR1, ABCB1), breast cancer
resistance protein (BCRP, ABCG2) and multidrug resistance protein 2 (MRP2, ABCC2) are …
resistance protein (BCRP, ABCG2) and multidrug resistance protein 2 (MRP2, ABCC2) are …
Restricted brain penetration of the tyrosine kinase inhibitor erlotinib due to the drug transporters P-gp and BCRP
NA de Vries, T Buckle, J Zhao, JH Beijnen… - Investigational new …, 2012 - Springer
Summary Purpose Erlotinib (Tarceva®, OSI-774) is a small molecule inhibitor of the
epidermal growth factor receptor (EGFR) tyrosine kinase. As high-grade gliomas frequently …
epidermal growth factor receptor (EGFR) tyrosine kinase. As high-grade gliomas frequently …
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