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Medline ® Abstract for Reference 218

of '肝病患者的化疗肝毒性和剂量调整'

218
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An open-label study to describe pharmacokinetic parameters of erlotinib in patients with advanced solid tumors with adequate and moderately impaired hepatic function.
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O'Bryant CL, Haluska P, Rosen L, Ramanathan RK, Venugopal B, Leong S, Boinpally R, Franke A, Witt K, Evans J, Belani C, Gail Eckhardt S, Ramalingam S
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Cancer Chemother Pharmacol. 2012 Mar;69(3):605-12. Epub 2011 Sep 22.
 
PURPOSE: To compare the pharmacokinetic (PK) parameters of a single dose of erlotinib in cancer patients with moderate hepatic impairment (MHI) to those of cancer patients with adequate hepatic function (AHF).
METHODS: Cancer patients with either AHF or MHI were treated with a single 150 mg dose of erlotinib on day 1 only followed by 96 h of plasma sampling for PK assessment. From day 5, patients were allowed to continue daily erlotinib in a maintenance phase. Non-smoking patients were stratified into an AHF cohort (total bilirubin ≤ upper limit of normal [ULN]and ALT/AST ≤ 1.5 X ULN) or a MHI cohort (Child-Pugh score of 7-9). The frequency of adverse events and laboratory changes were assessed.
RESULTS: Thirty-six patients, 21 with AHF and 15 with MHI, received at least onedose of erlotinib. The PK of erlotinib was similar between the two cohorts with a median C (max) of 1.09 versus 0.828 μg/mL and corresponding median AUC(0-t ) 29.3 versus 30.5 μg h/mL for the AHF and MHI cohorts, respectively. Adverse events from erlotinib in cancer patients with MHI were consistent with the known safety profile.
CONCLUSIONS: The PK and safety profiles of erlotinib in patients with MHI were similar to those with AHF. As a result, a reduced starting dose of erlotinib in patients with MHI is not required and treatment should be guided by patients' tolerability.
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Department of Clinical Pharmacy, School of Pharmacy, University of Colorado Cancer Center, Mail Stop C238, 12850 East Montview Blvd., V20-1223, Aurora, CO, 80045, USA. Cindy.OBryant@ucdenver.edu
PMID