Role of P-Glycoprotein and Breast Cancer Resistance Protein-1 in the Brain Penetration and Brain Pharmacodynamic Activity of the Novel Phosphatidylinositol 3-Kinase Inhibitor GDC-0941

Laurent Salphati; Leslie B. Lee; Jodie Pang; Emile G. Plise; Xiaolin Zhang

doi:10.1124/dmd.110.034256

Role of P-Glycoprotein and Breast Cancer Resistance Protein-1 in the Brain Penetration and Brain Pharmacodynamic Activity of the Novel Phosphatidylinositol 3-Kinase Inhibitor GDC-0941

Drug Metabolism and Disposition ◽

10.1124/dmd.110.034256 ◽

2010 ◽

Vol 38 (9) ◽

pp. 1422-1426 ◽

Cited By ~ 21

Author(s):

Laurent Salphati ◽

Leslie B. Lee ◽

Jodie Pang ◽

Emile G. Plise ◽

Xiaolin Zhang

Keyword(s):

Breast Cancer Resistance Protein ◽

Kinase Inhibitor ◽

The Novel ◽

Cancer Resistance ◽

Phosphatidylinositol 3 Kinase ◽

Brain Penetration ◽

P Glycoprotein ◽

Resistance Protein ◽

The Brain

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P-Glycoprotein and Breast Cancer Resistance Protein: Two Dominant Transporters Working Together in Limiting the Brain Penetration of Topotecan

Clinical Cancer Research ◽

10.1158/1078-0432.ccr-07-1335 ◽

2007 ◽

Vol 13 (21) ◽

pp. 6440-6449 ◽

Cited By ~ 172

Author(s):

Nienke A. de Vries ◽

Jin Zhao ◽

Emily Kroon ◽

Tessa Buckle ◽

Jos H. Beijnen ◽

...

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

Brain Penetration ◽

P Glycoprotein ◽

Working Together ◽

Resistance Protein ◽

The Brain

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Faculty Opinions recommendation of The effect of breast cancer resistance protein and P-glycoprotein on the brain penetration of flavopiridol, imatinib mesylate (Gleevec), prazosin, and 2-methoxy-3-(4-(2-(5-methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)propanoic acid (PF-407288) in mice.

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

10.3410/f.1157296.617432 ◽

2009 ◽

Author(s):

Susan Bates

Keyword(s):

Breast Cancer ◽

Imatinib Mesylate ◽

Breast Cancer Resistance Protein ◽

Propanoic Acid ◽

Cancer Resistance ◽

Brain Penetration ◽

P Glycoprotein ◽

Resistance Protein ◽

The Brain

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The Effect of Breast Cancer Resistance Protein and P-Glycoprotein on the Brain Penetration of Flavopiridol, Imatinib Mesylate (Gleevec), Prazosin, and 2-Methoxy-3-(4-(2-(5-methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)propanoic Acid (PF-407288) in Mice

Drug Metabolism and Disposition ◽

10.1124/dmd.108.024489 ◽

2009 ◽

Vol 37 (5) ◽

pp. 946-955 ◽

Cited By ~ 104

Author(s):

Lin Zhou ◽

Kari Schmidt ◽

Frederick R. Nelson ◽

Veronica Zelesky ◽

Matthew D. Troutman ◽

...

Keyword(s):

Breast Cancer ◽

Imatinib Mesylate ◽

Breast Cancer Resistance Protein ◽

Propanoic Acid ◽

Cancer Resistance ◽

Brain Penetration ◽

P Glycoprotein ◽

Resistance Protein ◽

The Brain

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The Effect of Bcrp1 (Abcg2) on the In vivo Pharmacokinetics and Brain Penetration of Imatinib Mesylate (Gleevec): Implications for the Use of Breast Cancer Resistance Protein and P-Glycoprotein Inhibitors to Enable the Brain Penetration of Imatinib in Patients

Cancer Research ◽

10.1158/0008-5472.can-04-2416 ◽

2005 ◽

Vol 65 (7) ◽

pp. 2577-2582 ◽

Cited By ~ 242

Author(s):

Pauline Breedveld ◽

Dick Pluim ◽

Greta Cipriani ◽

Peter Wielinga ◽

Olaf van Tellingen ◽

...

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

Brain Penetration ◽

P Glycoprotein ◽

Resistance Protein ◽

Glycoprotein Inhibitors ◽

The Brain ◽

In Vivo Pharmacokinetics

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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 P-glycoprotein and breast cancer resistance protein: two dominant transporters working together in limiting the brain penetration of topotecan.

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

10.3410/f.1103419.559468 ◽

2008 ◽

Author(s):

Susan Bates

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

Brain Penetration ◽

P Glycoprotein ◽

Working Together ◽

Resistance Protein ◽

The Brain

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P-glycoprotein and breast cancer resistance protein restrict the brain penetration of the CDK4/6 inhibitor palbociclib

Investigational New Drugs ◽

10.1007/s10637-015-0266-y ◽

2015 ◽

Vol 33 (5) ◽

pp. 1012-1019 ◽

Cited By ~ 35

Author(s):

Mark C. de Gooijer ◽

Ping Zhang ◽

Nishita Thota ◽

Isabel Mayayo-Peralta ◽

Levi C. M. Buil ◽

...

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

Brain Penetration ◽

P Glycoprotein ◽

Resistance Protein ◽

The Brain

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P‐glycoprotein (ABCB1) and Breast Cancer Resistance Protein (ABCG2) restrict the brain penetration of the Janus family of tyrosine kinase (JAK) inhibitor CYT387

The FASEB Journal ◽

10.1096/fasebj.27.1_supplement.1103.1 ◽

2013 ◽

Vol 27 (S1) ◽

Author(s):

Selvi Durmus ◽

Ning Xu ◽

Rolf W Sparidans ◽

Els Wagenaar ◽

Jos H Beijnen ◽

...

Keyword(s):

Breast Cancer ◽

Tyrosine Kinase ◽

Breast Cancer Resistance Protein ◽

Jak Inhibitor ◽

Cancer Resistance ◽

Brain Penetration ◽

P Glycoprotein ◽

Resistance Protein ◽

The Brain

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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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P-Glycoprotein and Breast Cancer Resistance Protein Restrict Apical-to-Basolateral Permeability of Human Brain Endothelium to Amyloid-β

Journal of Cerebral Blood Flow & Metabolism ◽

10.1038/jcbfm.2009.42 ◽

2009 ◽

Vol 29 (6) ◽

pp. 1079-1083 ◽

Cited By ~ 73

Author(s):

Leon M Tai ◽

A Jane Loughlin ◽

David K Male ◽

Ignacio A Romero

Keyword(s):

Breast Cancer ◽

Human Brain ◽

Breast Cancer Resistance Protein ◽

Amyloid Β ◽

Cancer Resistance ◽

Glycoprotein P ◽

P Glycoprotein ◽

Resistance Protein ◽

The Brain

The clearance of amyloid beta (Aβ) from the brain represents a novel therapeutic target for Alzheimer's disease. Conflicting data exist regarding the contribution of adenosine triphosphatebinding cassette transporters to the clearance of Aβ through the blood-brain barrier. Therefore, we investigated whether Aβ could be a substrate for P-glycoprotein (P-gp) and/or for breast cancer resistance protein (BCRP) using a human brain endothelial cell line, hCMEC/D3. Inhibition of P-gp and BCRP increased apical-to-basolateral, but not basolateral-to-apical, permeability of hCMEC/D3 cells to 125l Aβ 1–40. Our in vitro data suggest that P-gp and BCRP might act to prevent the blood-borne Aβ 1–40 from entering the brain.

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