P-glycoprotein and breast cancer resistance protein restrict brigatinib brain accumulation and toxicity, and, alongside CYP3A, limit its oral availability

Pharmacological Research ◽

10.1016/j.phrs.2018.09.020 ◽

2018 ◽

Vol 137 ◽

pp. 47-55 ◽

Author(s):

Wenlong Li ◽

Rolf W. Sparidans ◽

Yaogeng Wang ◽

Maria C. Lebre ◽

Jos H. Beijnen ◽

...

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

P Glycoprotein ◽

Resistance Protein ◽

Oral Availability

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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

Molecular Pharmaceutics ◽

10.1021/mp3003144 ◽

2012 ◽

Vol 9 (11) ◽

pp. 3236-3245 ◽

Author(s):

Selvi Durmus ◽

Rolf W. Sparidans ◽

Els Wagenaar ◽

Jos H. Beijnen ◽

Alfred H. Schinkel

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

Brain Penetration ◽

P Glycoprotein ◽

Resistance Protein ◽

Oral Availability

Download Full-text

Faculty Opinions recommendation of 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.

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

10.3410/f.718013225.793477286 ◽

2013 ◽

Author(s):

Susan Bates

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

Brain Penetration ◽

P Glycoprotein ◽

Resistance Protein ◽

Oral Availability

Download Full-text

Increased oral availability and brain accumulation of the ALK inhibitor crizotinib by coadministration of the P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar

International Journal of Cancer ◽

10.1002/ijc.28475 ◽

2013 ◽

Vol 134 (6) ◽

pp. 1484-1494 ◽

Author(s):

Seng Chuan Tang ◽

Luan N. Nguyen ◽

Rolf W. Sparidans ◽

Els Wagenaar ◽

Jos H. Beijnen ◽

...

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

Alk Inhibitor ◽

P Glycoprotein ◽

Resistance Protein ◽

Oral Availability

Download Full-text

Faculty Opinions recommendation of Breast cancer resistance protein (BCRP/ABCG2) and P-glycoprotein (P-gp/ABCB1) transport afatinib and restrict its oral availability and brain accumulation.

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

10.3410/f.727409671.793569213 ◽

2020 ◽

Author(s):

Michael Gottesman

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

Glycoprotein P ◽

P Glycoprotein ◽

Resistance Protein ◽

Oral Availability

Download Full-text

Faculty Opinions recommendation of P-glycoprotein and breast cancer resistance protein restrict brigatinib brain accumulation and toxicity, and, alongside CYP3A, limit its oral availability.

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

10.3410/f.734076177.793556597 ◽

2019 ◽

Author(s):

Susan Bates

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

P Glycoprotein ◽

Resistance Protein ◽

Oral Availability

Download Full-text

Abstract 5218: Breast cancer resistance protein (ABCG2) and P-glycoprotein (ABCB1) transport ibrutinib and may restrict its oral availability and brain accumulation, whereas CYP3A4 limits ibrutinib oral availability

10.1158/1538-7445.am2017-5218 ◽

2017 ◽

Author(s):

Stephanie van Hoppe ◽

Gert-Jan Rood ◽

Els Wagenaar ◽

Rolf Sparidans ◽

Jos Beijnen ◽

...

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

P Glycoprotein ◽

Resistance Protein ◽

Oral Availability

Download Full-text

Breast Cancer Resistance Protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1) Restrict Oral Availability and Brain Accumulation of the PARP Inhibitor Rucaparib (AG-014699)

Pharmaceutical Research ◽

10.1007/s11095-014-1442-z ◽

2014 ◽

Vol 32 (1) ◽

pp. 37-46 ◽

Author(s):

Selvi Durmus ◽

Rolf W. Sparidans ◽

Anita van Esch ◽

Els Wagenaar ◽

Jos H. Beijnen ◽

...

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Parp Inhibitor ◽

Cancer Resistance ◽

Glycoprotein P ◽

P Glycoprotein ◽

Resistance Protein ◽

Oral Availability

Download Full-text

Breast cancer resistance protein (BCRP/ABCG2) and P-glycoprotein (P-gp/ABCB1) transport afatinib and restrict its oral availability and brain accumulation

Pharmacological Research ◽

10.1016/j.phrs.2017.01.035 ◽

2017 ◽

Vol 120 ◽

pp. 43-50 ◽

Author(s):

Stéphanie van Hoppe ◽

Rolf W. Sparidans ◽

Els Wagenaar ◽

Jos H. Beijnen ◽

Alfred H. Schinkel

Keyword(s):

Breast Cancer ◽

Breast Cancer Resistance Protein ◽

Cancer Resistance ◽

Glycoprotein P ◽

P Glycoprotein ◽

Resistance Protein ◽

Oral Availability

Download Full-text

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 ◽

Download Full-text

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

Download Full-text