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Cancer Chemotherapy and Pharmacology

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01.07.2014 | Original Article

Irinotecan and temozolomide brain distribution: a focus on ABCB1

verfasst von: Lauriane Goldwirt, Kevin Beccaria, Alexandre Carpentier, Robert Farinotti, Christine Fernandez

Erschienen in: Cancer Chemotherapy and Pharmacology | Ausgabe 1/2014

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Abstract

Glioblastoma (GBM), the most common primary brain tumor in adults, is usually rapidly fatal with median survival duration of only 15 months and a 3-year survival rate of <7 %. Temozolomide (TMZ) is the only anticancer drug that has improved survival in GBM when administered with concomitant radiotherapy. Irinotecan (CPT-11) has also shown efficacy in recurrent gliomas monotherapy with moderate response. As the efficacy of GBM treatments relies on their brain distribution through the blood–brain barrier (BBB), the aim of the present work was to study, on an in vivo model, the brain distribution of TMZ, CPT-11 and its active metabolite, SN-38. We have focussed on the role of ABCB1, the main efflux transporter at the BBB level, through pharmacokinetics studies in CF1 mdr1a (+/+) and mdr1a (−/−) mice. Our results show that TMZ, CPT-11 and SN-38 are transported by ABCB1 at the BBB level with brain/plasma ratios of 1.1, 2.1 and 2.3, respectively.

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Titel: Irinotecan and temozolomide brain distribution: a focus on ABCB1
verfasst von: Lauriane Goldwirt
Kevin Beccaria
Alexandre Carpentier
Robert Farinotti
Christine Fernandez
Publikationsdatum: 01.07.2014
Verlag: Springer Berlin Heidelberg
Erschienen in: Cancer Chemotherapy and Pharmacology / Ausgabe 1/2014
Print ISSN: 0344-5704
Elektronische ISSN: 1432-0843
DOI: https://doi.org/10.1007/s00280-014-2490-0

Springer Medizin

Irinotecan and temozolomide brain distribution: a focus on ABCB1

Abstract

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Springer Medizin

Abstract

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