Binding of gefitinib, an inhibitor of epidermal growth factor receptor-tyrosine kinase, to plasma proteins and blood cells: in vitro and in cancer patients

J Li, J Brahmer, W Messersmith, M Hidalgo… - Investigational new …, 2006 - Springer
Gefitinib exhibits wide inter-subject pharmacokinetic variability which may contribute to
differences in treatment outcome. Unbound drug concentrations are believed to be more …

Single-dose clinical pharmacokinetic studies of gefitinib

HC Swaisland, RP Smith, A Laight, DJ Kerr… - Clinical …, 2005 - Springer
Background The objective of the five clinical studies presented in this article was to
investigate the single-dose pharmacokinetics of gefitinib (IRESSA®, ZD1839), an epidermal …

Specific method for determination of gefitinib in human plasma, mouse plasma and tissues using high performance liquid chromatography coupled to tandem mass …

M Zhao, C Hartke, A Jimeno, J Li, P He… - … of chromatography B, 2005 - Elsevier
A rapid, sensitive and specific method was developed and validated using liquid
chromatography–tandem mass spectrometry (LC/MS/MS) for determination of gefitinib in …

Tumor penetration of gefitinib (Iressa), an epidermal growth factor receptor tyrosine kinase inhibitor

D McKillop, EA Partridge, JV Kemp, MP Spence… - Molecular cancer …, 2005 - AACR
The relative distribution of gefitinib-related material in nude mice bearing sc human tumor
xenografts and in an orthotopic rat lung tumor model was investigated following oral …

Pharmacokinetics of gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, in rat and dog

D McKillop, EA Partridge, M Hutchison, SA Rhead… - Xenobiotica, 2004 - Taylor & Francis
1. The pharmacokinetics of gefitinib and its metabolites in rat and dog were investigated in
preclinical studies conducted to support the safety evaluation and clinical development of …

Functional characterization of gefitinib uptake in non-small cell lung cancer cell lines

M Galetti, RR Alfieri, A Cavazzoni, S La Monica… - Biochemical …, 2010 - Elsevier
Gefitinib, an inhibitor of epidermal growth factor receptor tyrosine kinase, has been
developed and approved for treatment of advanced non-small cell lung cancer (NSCLC). In …

Minimal contribution of desmethyl-gefitinib, the major human plasma metabolite of gefitinib, to epidermal growth factor receptor (EGFR)-mediated tumour growth …

D McKillop, SP Guy, MP Spence, J Kendrew… - Xenobiotica, 2006 - Taylor & Francis
Desmethyl-gefitinib is a major metabolite of gefitinib observed in human plasma at
concentrations similar to those of gefitinib. The epidermal growth factor receptor (EGFR) …

Pharmacokinetics of gefitinib: roles of drug metabolizing enzymes and transporters

C Zhao, SY Han, PP Li - Current drug delivery, 2017 - ingentaconnect.com
Gefitinib (Iressa, AstraZeneca) has been widely used for the treatment of locally advanced or
metastatic non-small cell lung cancer. A number of studies have been reported on its …

A simple HPLC-UV method for the simultaneous quantification of gefitinib and erlotinib in human plasma

L Faivre, C Gomo, O Mir, F Taieb… - … of Chromatography B, 2011 - Elsevier
Gefitinib and erlotinib are two oral tyrosine kinase inhibitors (TKI) approved for the treatment
of advanced non-small cell lung cancer (NSCLC). Published methods for simultaneous …

The effect of different etiologies of hepatic impairment on the pharmacokinetics of gefitinib

J Horak, J White, AL Harris, M Verrill… - Cancer chemotherapy …, 2011 - Springer
Purpose We investigated whether the pharmacokinetics and tolerability of gefitinib were
altered in patients with hepatic impairment due to cirrhosis or hepatic metastases in two …