Modulation of erlotinib pharmacokinetics in mice by a novel cytochrome P450 3A4 inhibitor, BAS 100

N. F. Smith; S. D. Baker; F. J. Gonzalez; J. W. Harris; W. D. Figg; A. Sparreboom

doi:10.1038/sj.bjc.6604353

Modulation of erlotinib pharmacokinetics in mice by a novel cytochrome P450 3A4 inhibitor, BAS 100

N. F. Smith
, S. D. Baker
, F. J. Gonzalez
, J. W. Harris
, W. D. Figg
, A. Sparreboom

Surgery

Research output: Contribution to journal › Article › peer-review

27 Scopus citations

Abstract

Administration of BAS 100, a novel mechanism-based CYP3A4 inhibitor isolated from grapefruit juice, resulted in a 2.1-fold increase in erlotinib exposure following oral administration to wild-type and humanised CYP3A4 transgenic mice. This study illustrates the potential of BAS 100 to increase the low and variable oral bioavailability of erlotinib in cancer patients.

Original language	English
Pages (from-to)	1630-1632
Number of pages	3
Journal	British Journal of Cancer
Volume	98
Issue number	10
DOIs	https://doi.org/10.1038/sj.bjc.6604353
State	Published - 20 May 2008

Keywords

CYP3A4 transgenic
Grapefruit
Metabolism
OSI-420
OSI-774
Tarceva

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title = "Modulation of erlotinib pharmacokinetics in mice by a novel cytochrome P450 3A4 inhibitor, BAS 100",

abstract = "Administration of BAS 100, a novel mechanism-based CYP3A4 inhibitor isolated from grapefruit juice, resulted in a 2.1-fold increase in erlotinib exposure following oral administration to wild-type and humanised CYP3A4 transgenic mice. This study illustrates the potential of BAS 100 to increase the low and variable oral bioavailability of erlotinib in cancer patients.",

keywords = "CYP3A4 transgenic, Grapefruit, Metabolism, OSI-420, OSI-774, Tarceva",

author = "Smith, \{N. F.\} and Baker, \{S. D.\} and Gonzalez, \{F. J.\} and Harris, \{J. W.\} and Figg, \{W. D.\} and A. Sparreboom",

note = "Funding Information: This research was supported by the Intramural Research Program of the NIH, National Cancer Institute, Center for Cancer Research (Bethesda, MD, USA). We thank Dr Linda G Byrd (Laboratory of Metabolism, Centre for Cancer Research, National Cancer Institute, Bethesda, MD, USA) for assistance with the CYP3A4 transgenic mouse study and Dr Ming Zhao (Johns Hopkins",

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doi = "10.1038/sj.bjc.6604353",

language = "English",

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AU - Baker, S. D.

AU - Gonzalez, F. J.

AU - Harris, J. W.

AU - Figg, W. D.

AU - Sparreboom, A.

N1 - Funding Information: This research was supported by the Intramural Research Program of the NIH, National Cancer Institute, Center for Cancer Research (Bethesda, MD, USA). We thank Dr Linda G Byrd (Laboratory of Metabolism, Centre for Cancer Research, National Cancer Institute, Bethesda, MD, USA) for assistance with the CYP3A4 transgenic mouse study and Dr Ming Zhao (Johns Hopkins

PY - 2008/5/20

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N2 - Administration of BAS 100, a novel mechanism-based CYP3A4 inhibitor isolated from grapefruit juice, resulted in a 2.1-fold increase in erlotinib exposure following oral administration to wild-type and humanised CYP3A4 transgenic mice. This study illustrates the potential of BAS 100 to increase the low and variable oral bioavailability of erlotinib in cancer patients.

AB - Administration of BAS 100, a novel mechanism-based CYP3A4 inhibitor isolated from grapefruit juice, resulted in a 2.1-fold increase in erlotinib exposure following oral administration to wild-type and humanised CYP3A4 transgenic mice. This study illustrates the potential of BAS 100 to increase the low and variable oral bioavailability of erlotinib in cancer patients.

KW - CYP3A4 transgenic

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KW - Metabolism

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KW - OSI-774

KW - Tarceva

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M3 - Article

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JO - British Journal of Cancer

JF - British Journal of Cancer

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ER -

Modulation of erlotinib pharmacokinetics in mice by a novel cytochrome P450 3A4 inhibitor, BAS 100

Abstract

Keywords

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