Saturable Active Efflux by P-Glycoprotein and Breast Cancer Resistance Protein at the Blood-Brain Barrier Leads to Nonlinear Distribution of Elacridar to the Central Nervous System

Ramola Sane; Sagar Agarwal; Rajendar K. Mittapalli; William F. Elmquist

doi:10.1124/jpet.112.199786

Saturable Active Efflux by P-Glycoprotein and Breast Cancer Resistance Protein at the Blood-Brain Barrier Leads to Nonlinear Distribution of Elacridar to the Central Nervous System

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.112.199786 ◽

2013 ◽

Vol 345 (1) ◽

pp. 111-124 ◽

Cited By ~ 26

Author(s):

Ramola Sane ◽

Sagar Agarwal ◽

Rajendar K. Mittapalli ◽

William F. Elmquist

Keyword(s):

Breast Cancer ◽

Central Nervous System ◽

Nervous System ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

Active Efflux ◽

P Glycoprotein ◽

The Central Nervous System ◽

Resistance Protein ◽

Nonlinear Distribution

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ATP-binding cassette transporters in primary central nervous system lymphoma: Decreased expression of MDR1 P-glycoprotein and breast cancer resistance protein in tumor capillary endothelial cells

Oncology Reports ◽

10.3892/or.2010.1102 ◽

2011 ◽

Vol 25 (2) ◽

Author(s):

Fujiwara

Keyword(s):

Breast Cancer ◽

Central Nervous System ◽

Nervous System ◽

Breast Cancer Resistance Protein ◽

Central Nervous System Lymphoma ◽

Cancer Resistance ◽

P Glycoprotein ◽

Atp Binding Cassette Transporters ◽

Capillary Endothelial Cells ◽

Resistance Protein

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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): TABLE 1

Drug Metabolism and Disposition ◽

10.1124/dmd.108.024646 ◽

2008 ◽

Vol 37 (2) ◽

pp. 439-442 ◽

Cited By ~ 174

Author(s):

Joseph W. Polli ◽

Katie L. Olson ◽

John P. Chism ◽

Lisa St. John-Williams ◽

Russell L. Yeager ◽

...

Keyword(s):

Breast Cancer ◽

Central Nervous System ◽

Breast Cancer Resistance Protein ◽

Kinase Inhibitor ◽

Cancer Resistance ◽

P Glycoprotein ◽

Central Nervous System Penetration ◽

The Central Nervous System ◽

Resistance Protein

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Faculty Opinions recommendation of Distribution of gefitinib to the brain is limited by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2)-mediated active efflux.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.3171959.2859057 ◽

2010 ◽

Author(s):

Susan Bates

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

Active Efflux ◽

P Glycoprotein ◽

Resistance Protein ◽

The Brain

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Absence of both MDR1 (ABCB1) and Breast Cancer Resistance Protein (ABCG2) Transporters Significantly Alters Rivaroxaban Disposition and Central Nervous System Entry

Basic & Clinical Pharmacology & Toxicology ◽

10.1111/bcpt.12005 ◽

2012 ◽

Vol 112 (3) ◽

pp. 164-170 ◽

Cited By ~ 24

Author(s):

Inna Y. Gong ◽

Sara E. Mansell ◽

Richard B. Kim

Keyword(s):

Breast Cancer ◽

Central Nervous System ◽

Nervous System ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

Resistance Protein

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Investigation of the Role of Breast Cancer Resistance Protein (Bcrp/Abcg2) on Pharmacokinetics and Central Nervous System Penetration of Abacavir and Zidovudine in the Mouse

Drug Metabolism and Disposition ◽

10.1124/dmd.108.020974 ◽

2008 ◽

Vol 36 (8) ◽

pp. 1476-1484 ◽

Cited By ~ 49

Author(s):

Nagdeep Giri ◽

Naveed Shaik ◽

Guoyu Pan ◽

Tetsuya Terasaki ◽

Chisato Mukai ◽

...

Keyword(s):

Breast Cancer ◽

Central Nervous System ◽

Nervous System ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

Central Nervous System Penetration ◽

Resistance Protein

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Quantitative Evaluation of the Impact of Active Efflux by P-Glycoprotein and Breast Cancer Resistance Protein at the Blood-Brain Barrier on the Predictability of the Unbound Concentrations of Drugs in the Brain Using Cerebrospinal Fluid Concentration as a Surrogate

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.111.180398 ◽

2011 ◽

Vol 339 (3) ◽

pp. 935-944 ◽

Cited By ~ 73

Author(s):

Hiroshi Kodaira ◽

Hiroyuki Kusuhara ◽

Takuya Fujita ◽

Junko Ushiki ◽

Eiichi Fuse ◽

...

Keyword(s):

Breast Cancer ◽

Cerebrospinal Fluid ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

Active Efflux ◽

P Glycoprotein ◽

Fluid Concentration ◽

Resistance Protein ◽

The Impact ◽

The Brain

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Distribution of Gefitinib to the Brain Is Limited by P-glycoprotein (ABCB1) and Breast Cancer Resistance Protein (ABCG2)-Mediated Active Efflux

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.110.167601 ◽

2010 ◽

Vol 334 (1) ◽

pp. 147-155 ◽

Cited By ~ 156

Author(s):

Sagar Agarwal ◽

Ramola Sane ◽

Jose L. Gallardo ◽

John R. Ohlfest ◽

William F. Elmquist

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

Active Efflux ◽

P Glycoprotein ◽

Resistance Protein ◽

The Brain

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Faculty Opinions recommendation of Brain accumulation of the EML4-ALK inhibitor ceritinib is restricted by P-glycoprotein (P-GP/ABCB1) and breast cancer resistance protein (BCRP/ABCG2).

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.725783242.793517907 ◽

2016 ◽

Author(s):

Susan Bates

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

Glycoprotein P ◽

Alk Inhibitor ◽

P Glycoprotein ◽

Resistance Protein

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Faculty of 1000 evaluation for The "specific" P-glycoprotein inhibitor tariquidar is also a substrate and an inhibitor for breast cancer resistance protein (BCRP/ABCG2).

F1000 - Post-publication peer review of the biomedical literature ◽

10.3410/f.9419956.10057054 ◽

2011 ◽

Author(s):

Robert Fecik

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

P Glycoprotein ◽

Resistance Protein

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Optimization of dose and route of administration of the P‐glycoprotein inhibitor, valspodar (PSC‐833) and the P‐glycoprotein and breast cancer resistance protein dual‐inhibitor, elacridar (GF120918) as dual infusion in rats

Pharmacology Research & Perspectives ◽

10.1002/prp2.740 ◽

2021 ◽

Vol 9 (2) ◽

Author(s):

Christopher Rowbottom ◽

Alicia Pietrasiewics ◽

Taras Tuczewycz ◽

Richard Grater ◽

Daniel Qiu ◽

...

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Route Of Administration ◽

Cancer Resistance ◽

Dual Inhibitor ◽

Psc 833 ◽

P Glycoprotein ◽

Resistance Protein

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