Matches in SemOpenAlex for { <https://semopenalex.org/work/W2096592200> ?p ?o ?g. }
- W2096592200 endingPage "528" @default.
- W2096592200 startingPage "520" @default.
- W2096592200 abstract "Edoxaban (the free base of DU-176b), an oral direct factor Xa inhibitor, is mainly excreted unchanged into urine and feces. Because active membrane transport processes such as active renal secretion, biliary excretion, and/or intestinal secretion, and the incomplete absorption of edoxaban after oral administration have been observed, the involvement of drug transporters in the disposition of edoxaban was investigated. Using a bidirectional transport assay in human colon adenocarcinoma Caco-2 cell monolayers, we observed the vectorial transport of [<sup>14</sup>C]edoxaban, which was completely inhibited by verapamil, a strong P-glycoprotein (P-gp) inhibitor. In an in vivo study, an increased distribution of edoxaban to the brain was observed in Mdr1a/1b knockout mice when compared with wild-type mice, indicating that edoxaban is a substrate for P-gp. However, there have been no observations of significant transport of edoxaban by renal or hepatic uptake transporters, organic anion transporter (OAT)1, OAT3, organic cation transporter (OCT)2, or organic anion transporting polypeptide (OATP)1B1. Edoxaban exhibited no remarkable inhibition of OAT1, OAT3, OCT1, OCT2, OATP1B1, OATP1B3, or P-gp up to 30 <i>μ</i>M; therefore, the risk of clinical drug–drug interactions due to any edoxaban-related transporter inhibition seems to be negligible. Our results demonstrate that edoxaban is a substrate of P-gp but not of other major uptake transporters tested. Because metabolism is a minor contributor to the total clearance of edoxaban and strong P-gp inhibitors clearly impact edoxaban transport, the P-gp transport system is a key factor for edoxaban’s disposition." @default.
- W2096592200 created "2016-06-24" @default.
- W2096592200 creator A5011947741 @default.
- W2096592200 creator A5024316557 @default.
- W2096592200 creator A5038047310 @default.
- W2096592200 creator A5059468376 @default.
- W2096592200 creator A5067065259 @default.
- W2096592200 creator A5073828535 @default.
- W2096592200 creator A5086826930 @default.
- W2096592200 creator A5087204052 @default.
- W2096592200 date "2014-01-23" @default.
- W2096592200 modified "2023-10-07" @default.
- W2096592200 title "Edoxaban Transport via P-Glycoprotein Is a Key Factor for the Drug’s Disposition" @default.
- W2096592200 cites W1783939843 @default.
- W2096592200 cites W1965320794 @default.
- W2096592200 cites W1971182486 @default.
- W2096592200 cites W1974709342 @default.
- W2096592200 cites W1978882295 @default.
- W2096592200 cites W1979024502 @default.
- W2096592200 cites W1992094709 @default.
- W2096592200 cites W2002119441 @default.
- W2096592200 cites W2015854890 @default.
- W2096592200 cites W2027735039 @default.
- W2096592200 cites W2039761330 @default.
- W2096592200 cites W2055518481 @default.
- W2096592200 cites W2079197876 @default.
- W2096592200 cites W2099823373 @default.
- W2096592200 cites W2113205708 @default.
- W2096592200 cites W2121703474 @default.
- W2096592200 cites W2151514200 @default.
- W2096592200 cites W2168993879 @default.
- W2096592200 cites W2172147566 @default.
- W2096592200 cites W2329886446 @default.
- W2096592200 doi "https://doi.org/10.1124/dmd.113.054866" @default.
- W2096592200 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24459178" @default.
- W2096592200 hasPublicationYear "2014" @default.
- W2096592200 type Work @default.
- W2096592200 sameAs 2096592200 @default.
- W2096592200 citedByCount "79" @default.
- W2096592200 countsByYear W20965922002014 @default.
- W2096592200 countsByYear W20965922002015 @default.
- W2096592200 countsByYear W20965922002016 @default.
- W2096592200 countsByYear W20965922002017 @default.
- W2096592200 countsByYear W20965922002018 @default.
- W2096592200 countsByYear W20965922002019 @default.
- W2096592200 countsByYear W20965922002020 @default.
- W2096592200 countsByYear W20965922002021 @default.
- W2096592200 countsByYear W20965922002022 @default.
- W2096592200 countsByYear W20965922002023 @default.
- W2096592200 crossrefType "journal-article" @default.
- W2096592200 hasAuthorship W2096592200A5011947741 @default.
- W2096592200 hasAuthorship W2096592200A5024316557 @default.
- W2096592200 hasAuthorship W2096592200A5038047310 @default.
- W2096592200 hasAuthorship W2096592200A5059468376 @default.
- W2096592200 hasAuthorship W2096592200A5067065259 @default.
- W2096592200 hasAuthorship W2096592200A5073828535 @default.
- W2096592200 hasAuthorship W2096592200A5086826930 @default.
- W2096592200 hasAuthorship W2096592200A5087204052 @default.
- W2096592200 hasConcept C104317684 @default.
- W2096592200 hasConcept C112705442 @default.
- W2096592200 hasConcept C123584848 @default.
- W2096592200 hasConcept C126322002 @default.
- W2096592200 hasConcept C133936738 @default.
- W2096592200 hasConcept C149011108 @default.
- W2096592200 hasConcept C185592680 @default.
- W2096592200 hasConcept C189613389 @default.
- W2096592200 hasConcept C2776301958 @default.
- W2096592200 hasConcept C2776678969 @default.
- W2096592200 hasConcept C2776769776 @default.
- W2096592200 hasConcept C2778707650 @default.
- W2096592200 hasConcept C2778810321 @default.
- W2096592200 hasConcept C2779161974 @default.
- W2096592200 hasConcept C2780290652 @default.
- W2096592200 hasConcept C501593827 @default.
- W2096592200 hasConcept C55493867 @default.
- W2096592200 hasConcept C71924100 @default.
- W2096592200 hasConcept C98274493 @default.
- W2096592200 hasConceptScore W2096592200C104317684 @default.
- W2096592200 hasConceptScore W2096592200C112705442 @default.
- W2096592200 hasConceptScore W2096592200C123584848 @default.
- W2096592200 hasConceptScore W2096592200C126322002 @default.
- W2096592200 hasConceptScore W2096592200C133936738 @default.
- W2096592200 hasConceptScore W2096592200C149011108 @default.
- W2096592200 hasConceptScore W2096592200C185592680 @default.
- W2096592200 hasConceptScore W2096592200C189613389 @default.
- W2096592200 hasConceptScore W2096592200C2776301958 @default.
- W2096592200 hasConceptScore W2096592200C2776678969 @default.
- W2096592200 hasConceptScore W2096592200C2776769776 @default.
- W2096592200 hasConceptScore W2096592200C2778707650 @default.
- W2096592200 hasConceptScore W2096592200C2778810321 @default.
- W2096592200 hasConceptScore W2096592200C2779161974 @default.
- W2096592200 hasConceptScore W2096592200C2780290652 @default.
- W2096592200 hasConceptScore W2096592200C501593827 @default.
- W2096592200 hasConceptScore W2096592200C55493867 @default.
- W2096592200 hasConceptScore W2096592200C71924100 @default.
- W2096592200 hasConceptScore W2096592200C98274493 @default.
- W2096592200 hasIssue "4" @default.
- W2096592200 hasLocation W20965922001 @default.