ArticleMolecular pharmaceutics2023
Dissimilar Effect of P-Glycoprotein and Breast Cancer Resistance Protein Inhibition on the Distribution of Erlotinib to the Retina and Brain in Humans and Mice.
Myriam El Biali, Sylvain Auvity, Salvatore Cisternino, Maria Smirnova, Marcus Hacker, Markus Zeitlinger, Severin Mairinger, Nicolas Tournier, Martin Bauer, Oliver Langer
Open access · hybridAbstract read
In one paragraphArticle in Molecular pharmaceutics, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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What it found
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2 · The registryThe trial behind it
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3 · Its place in the literatureWho cites it
0 citing papers in PubMed, 2 citations in OpenAlex.
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4 · The recordCorrections and comments
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5 · Who and what moneyAuthors and funding
10 authors at 4 institutions in 2 countries.
Myriam El BialiDepartment of Clinical Pharmacology, Medical University of Vienna, 1090 Vienna, Austria.
Sylvain AuvityInserm UMRS1144, Optimisation Thérapeutique en Neuropsychopharmacologie, Université Paris Cité, F-75006 Paris, France.
Salvatore CisterninoInserm UMRS1144, Optimisation Thérapeutique en Neuropsychopharmacologie, Université Paris Cité, F-75006 Paris, France.
Maria SmirnovaInserm UMRS1144, Optimisation Thérapeutique en Neuropsychopharmacologie, Université Paris Cité, F-75006 Paris, France.
Marcus HackerDivision of Nuclear Medicine, Department of Biomedical Imaging and Image-guided Therapy, Medical University of Vienna, 1090 Vienna, Austria.
Markus ZeitlingerDepartment of Clinical Pharmacology, Medical University of Vienna, 1090 Vienna, Austria.
Severin MairingerDepartment of Clinical Pharmacology, Medical University of Vienna, 1090 Vienna, Austria.
Nicolas TournierLaboratoire d'Imagerie Biomédicale Multimodale (BioMaps), CEA, CNRS, Inserm, Service Hospitalier Frédéric Joliot, Université Paris-Saclay, 91401 Orsay, France.
Martin BauerDepartment of Clinical Pharmacology, Medical University of Vienna, 1090 Vienna, Austria.
Oliver LangerDepartment of Clinical Pharmacology, Medical University of Vienna, 1090 Vienna, Austria.ORCID 0000-0002-4048-5781 Medical University of Vienna · ATHôpital Necker-Enfants Malades · FRCentre National de la Recherche Scientifique · FRInserm · FR
Funding
Austrian Science Fund FWF I 4470
6 · The paper itselfAbstract
P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) are two ATP-binding cassette efflux transporters that are coexpressed at the human blood-brain barrier (BBB) and blood-retina barrier (BRB). While pharmacological inhibition of P-gp and/or BCRP results in increased brain distribution of dual P-gp/BCRP substrate drugs, such as the tyrosine kinase inhibitor erlotinib, the effect of P-gp and/or BCRP inhibition on the retinal distribution of such drugs has hardly been investigated. In this study, we used positron emission tomography (PET) imaging to assess the effect of transporter inhibition on the distribution of [
Indexed as
ATP Binding Cassette Transporter, Subfamily B, Member 1Breast NeoplasmsAnimalsATP-Binding Cassette TransportersATP Binding Cassette Transporter, Subfamily BATP Binding Cassette Transporter, Subfamily G, Member 2Blood-Brain BarrierBlood-Retinal BarrierBrainErlotinib HydrochlorideFemaleHumansMembrane Transport ProteinsMiceNeoplasm ProteinsATP-Binding Cassette TransportersATP Binding Cassette Transporter, Subfamily BATP Binding Cassette Transporter, Subfamily B, Member 1ATP Binding Cassette Transporter, Subfamily G, Member 2Erlotinib HydrochlorideMembrane Transport ProteinsNeoplasm ProteinsBCRPblood-brain barrierblood-retina barriererlotinibhumansin situ carotid perfusionmicePETP-gptariquidar
Identifiers
PMID37883694
PMCPMC10630959
OpenAlexW4387965929
What OpenQuestion holds
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LicenceCC BY
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