CYP3A4, an important drug-metabolizing enzyme, is known to have genetic variants. In this study, we quantitatively investigated the inhibition kinetics of two typical inhibitors, itraconazole ITCZ and cimetidine CMD , on CYP3A4 variants and evaluated whether the genetic variation leads to interindividual differences in the extent of CYP3A4-mediated drug interactions. The genetic variation of CYP3A4 significantly affected the inhibition profiles of the two inhibitors. In CYP3A4. The influence of other genetic variations also differed between the two inhibitors. Docking simulations could explain the changes in the Ki values, based on the accessibility of TST and inhibitors to the heme moiety of the CYP3A4 molecule. In conclusion, the inhibitory effects of an inhibitor differ among CYP3A4 variants, suggesting that the genetic variation of CYP3A4 may contribute, at least in part, to interindividual differences in drug interactions mediated by CYP3A4 inhibition, and the pattern of the influences of genetic variation differs among inhibitors as well as substrates. Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P 3A4 genetic variants. T1 - Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P 3A4 genetic variants. N2 - CYP3A4, an important drug-metabolizing enzyme, is known to have genetic variants.
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Skip to search form Skip to main content. You are currently offline. Some features of the site may not work correctly. Medicine Published in International journal of…. PURPOSE In order to identify methods for preventing phlebitis caused by intravenous administration of vinorelbine VNR , we established a procedure for estimating the severity of phlebitis in an animal model. VNR was diluted with normal saline to prepare test solutions with concentrations of 0. View PDF. Save to Library. Create Alert. Share This Paper.
Skip to search form Skip to main content. You are currently offline. Some features of the site may not work correctly. Medicine Published in International journal of…. PURPOSE In order to identify methods for preventing phlebitis caused by intravenous administration of vinorelbine VNR , we established a procedure for estimating the severity of phlebitis in an animal model.
VNR was diluted with normal saline to prepare test solutions with concentrations of 0. View PDF. Save to Library. Create Alert. Share This Paper. Figures, Tables, and Topics from this paper.
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Randomized trial of drip infusion versus bolus injection of vinorelbine for the control of local venous toxicity. Gemcitabine and vinorelbine in recurrent advanced non-small cell lung cancer: sequence does matter Rosalyn A. Juergens , Julie R. Brahmer , David S. Ettinger Medicine Cancer Chemotherapy and Pharmacology Late phase II clinical study of vinorelbine monotherapy in advanced or recurrent breast cancer previously treated with anthracyclines and taxanes. Vinorelbine and venous irritation: optimal parenteral administration.
Prevention of vinorelbine phlebitis with cimetidine. A two-step design study. Orphanos , Anna P. Randomized phase III trial of paclitaxel plus carboplatin versus vinorelbine plus cisplatin in the treatment of patients with advanced non--small-cell lung cancer: a Southwest Oncology Group trial.
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