Contribution of OATP1B1 and OATP1B3 to the Disposition of Sorafenib and Sorafenib-Glucuronide
نویسندگان
چکیده
منابع مشابه
Cancer Therapy: Preclinical Contribution of OATP1B1 and OATP1B3 to the Disposition of Sorafenib and Sorafenib-Glucuronide
Purpose:Many tyrosine kinase inhibitors (TKI) undergo extensive hepaticmetabolism, butmechanisms of their hepatocellular uptake remain poorly understood. We hypothesized that liver uptake of TKIs is mediated by the solute carriers OATP1B1 and OATP1B3. Experimental Design: Transport of crizotinib, dasatinib, gefitinib, imatinib, nilotinib, pazopanib, sorafenib, sunitinib, vandetanib, and vemuraf...
متن کاملContribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide.
PURPOSE Many tyrosine kinase inhibitors (TKI) undergo extensive hepatic metabolism, but mechanisms of their hepatocellular uptake remain poorly understood. We hypothesized that liver uptake of TKIs is mediated by the solute carriers OATP1B1 and OATP1B3. EXPERIMENTAL DESIGN Transport of crizotinib, dasatinib, gefitinib, imatinib, nilotinib, pazopanib, sorafenib, sunitinib, vandetanib, and vemu...
متن کاملInfluence of OATP1B1 Function on the Disposition of Sorafenib‐β‐D‐Glucuronide
The oral multikinase inhibitor sorafenib undergoes extensive UGT1A9-mediated formation of sorafenib-β-D-glucuronide (SG). Using transporter-deficient mouse models, it was previously established that SG can be extruded into bile by ABCC2 or follow a liver-to-blood shuttling loop via ABCC3-mediated efflux into the systemic circulation, and subsequent uptake in neighboring hepatocytes by OATP1B-ty...
متن کاملCommentary on: “Influence of OATP1B1 Function on the Disposition of Sorafenib‐β‐D‐Glucuronide”
Approaches to predict and characterize drug–drug interactions (DDI) mediated by a single drug-metabolizing enzyme or a single transporter are well established. However, complex DDIs, where multiple metabolic and transport processes are involved, require an integrative translational approach.1,2 If a drug undergoes reversible metabolism, the net contribution of the processes of metabolism, uptak...
متن کاملcontribution of setting to the study of characters and the main idea in e. brontes: wuthering heights and t. hardys: return of the native.
this thesis aims to adduce an unmitigated and comprehensive explication concerning the relationship of three significant elements of fiction: setting, chracter and theme. my research is basically placed on two outstanding novels of the 19th century: emily brontes wuthering heights and thomas hardys return of the native. my endeavour lies in studying the correlation among the three above-mention...
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ژورنال
عنوان ژورنال: Clinical Cancer Research
سال: 2013
ISSN: 1078-0432,1557-3265
DOI: 10.1158/1078-0432.ccr-12-3306