{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,17]],"date-time":"2026-08-17T00:22:09Z","timestamp":1786926129373,"version":"build-2736575974"},"reference-count":25,"publisher":"Wiley","issue":"5","license":[{"start":{"date-parts":[[2015,1,14]],"date-time":"2015-01-14T00:00:00Z","timestamp":1421193600000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by-nc\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["The Journal of Clinical Pharma"],"published-print":{"date-parts":[[2015,5]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:sec><jats:label\/><jats:p>The effects of OATP1B1, OAT3, and MRP2 on the pharmacokinetics of eluxadoline, an oral, locally active, opioid receptor agonist\/antagonist being developed for treatment of IBS\u2010d were assessed in vivo. Coadministration of a single 200\u2009mg dose of eluxadoline with cyclosporine, and probenecid increased eluxadoline systemic exposure [AUC<jats:sub>(0\u2013inf)<\/jats:sub>] by 4.4\u2010 and 1.4\u2010fold, respectively, whereas peak exposure (C<jats:sub>max<\/jats:sub>) increased 6.2\u2010fold and 1.3\u2010fold, respectively. Cyclosporine had little effect on renal clearance (CL<jats:sub>ren<\/jats:sub>) of eluxadoline whereas probenecid reduced CL<jats:sub>ren<\/jats:sub> by nearly 50%. These study results suggested that sinusoidal OATP1B1\u2010mediated hepatic uptake of eluxadoline (during first\u2010pass and systemic extraction) plays a major role in its absorption and disposition, whereas OAT3\u2010mediated basolateral uptake in the proximal renal tubules and MRP2\u2010mediated canalicular and renal tubular apical efflux play only minor roles in its overall disposition. All treatments were safe and well tolerated.<\/jats:p><\/jats:sec>","DOI":"10.1002\/jcph.442","type":"journal-article","created":{"date-parts":[[2014,12,10]],"date-time":"2014-12-10T11:42:24Z","timestamp":1418211744000},"page":"534-542","source":"Crossref","is-referenced-by-count":39,"title":["Effect of uptake transporters OAT3 and OATP1B1 and efflux transporter MRP2 on the pharmacokinetics of eluxadoline"],"prefix":"10.1002","volume":"55","author":[{"given":"J. Michael","family":"Davenport","sequence":"first","affiliation":[{"name":"Furiex Pharmaceuticals Inc. Morrisville NC USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Paul","family":"Covington","sequence":"additional","affiliation":[{"name":"Furiex Pharmaceuticals Inc. Morrisville NC USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Laura","family":"Bonifacio","sequence":"additional","affiliation":[{"name":"Furiex Pharmaceuticals Inc. 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