0 26

Cited 22 times in

Increased systemic exposure of fimasartan, an angiotensin II receptor antagonist, by ketoconazole and rifampicin

DC FieldValueLanguage
dc.contributor.author이민구-
dc.date.accessioned2018-05-10T06:41:41Z-
dc.date.available2018-05-10T06:41:41Z-
dc.date.issued2013-
dc.identifier.issn0091-2700-
dc.identifier.urihttps://ir.ymlib.yonsei.ac.kr/handle/22282913/158445-
dc.description.abstractThe authors studied the effects of ketoconazole and rifampicin on the pharmacokinetics of a single dose of fimasartan (BR-A-657), a newly developed angiotensin II receptor antagonist for the treatment of hypertension, in 22 healthy participants. Ketoconazole increased the maximumplasma concentration (Cmax) and area under the plasma concentration vs time curve to infinity (AUC∞ of fimasartan by 2.47-fold (90% confidence interval [CI], 1.61-3.79) and 2.03-fold (1.56-2.64), respectively. Concomitant administration of rifampicin increased the C(max) and AUC∞ of fimasartan by 10.33-fold (90% CI, 6.74-15.81) and 4.60-fold (3.54-5.97). In vitro studies indicated that ketoconazole inhibited the uptake of fimasartan into cells expressing OATP1B1 with a K(i) of 107.7 µM, and rifampicin inhibited OAT1- and OATP1B1-mediated fimasartan transport with a K(i) of 212 µM and 12.2 µM, respectively. The systemic exposure of fimasartan was significantly increased by coadministration of ketoconazole or rifampicin in healthy volunteers. This is consistent with the in vitro results, in which fimasartan is a substrate of CYP3A and OATP1B1.-
dc.description.statementOfResponsibilityrestriction-
dc.languageEnglish-
dc.publisherWiley-
dc.relation.isPartOfJournal of Clinical Pharmacology-
dc.rightsCC BY-NC-ND 2.0 KR-
dc.rightshttps://creativecommons.org/licenses/by-nc-nd/2.0/kr/-
dc.subject.MESHAdult-
dc.subject.MESHAngiotensin II Type 1 Receptor Blockers/administration & dosage-
dc.subject.MESHAngiotensin II Type 1 Receptor Blockers/blood-
dc.subject.MESHAngiotensin II Type 1 Receptor Blockers/pharmacokinetics*-
dc.subject.MESHAnimals-
dc.subject.MESHArea Under Curve-
dc.subject.MESHBiphenyl Compounds/administration & dosage-
dc.subject.MESHBiphenyl Compounds/blood-
dc.subject.MESHBiphenyl Compounds/pharmacokinetics*-
dc.subject.MESHCells, Cultured-
dc.subject.MESHCross-Over Studies-
dc.subject.MESHDrug Interactions-
dc.subject.MESHHumans-
dc.subject.MESHKetoconazole/administration & dosage*-
dc.subject.MESHMale Oocytes/drug effects-
dc.subject.MESHOocytes/metabolism-
dc.subject.MESHOrganic Anion Transport Protein 1/genetics-
dc.subject.MESHOrganic Anion Transport Protein 1/metabolism-
dc.subject.MESHOrganic Anion Transporters/genetics-
dc.subject.MESHOrganic Anion Transporters/metabolism-
dc.subject.MESHPyrimidines/administration & dosage-
dc.subject.MESHPyrimidines/blood-
dc.subject.MESHPyrimidines/pharmacokinetics*-
dc.subject.MESHRifampin/administration & dosage*-
dc.subject.MESHSolute Carrier Organic Anion Transporter Family Member 1b1-
dc.subject.MESHTetrazoles/administration & dosage-
dc.subject.MESHTetrazoles/blood-
dc.subject.MESHTetrazoles/pharmacokinetics*-
dc.subject.MESHXenopus laevis-
dc.subject.MESHYoung Adult-
dc.titleIncreased systemic exposure of fimasartan, an angiotensin II receptor antagonist, by ketoconazole and rifampicin-
dc.typeArticle-
dc.contributor.collegeCollege of Medicine-
dc.contributor.departmentDept. of Pharmacology-
dc.contributor.googleauthorJung Won Kim-
dc.contributor.googleauthorSoJeong Yi-
dc.contributor.googleauthorTae-Eun Kim-
dc.contributor.googleauthorKyoung Soo Lim-
dc.contributor.googleauthorSeo Hyun Yoon-
dc.contributor.googleauthorJoo-Youn Cho-
dc.contributor.googleauthorMin Goo Lee-
dc.contributor.googleauthorIm-Sook Song-
dc.contributor.googleauthorSang-Goo Shin-
dc.contributor.googleauthorIn-Jin Jang-
dc.contributor.googleauthorKyung-Sang Yu-
dc.identifier.doi10.1177/0091270011433328-
dc.contributor.localIdA02781-
dc.relation.journalcodeJ01338-
dc.identifier.eissn1552-4604-
dc.identifier.pmid23400746-
dc.identifier.urlhttp://onlinelibrary.wiley.com/doi/10.1177/0091270011433328/abstract-
dc.contributor.alternativeNameLee, Min Goo-
dc.contributor.affiliatedAuthorLee, Min Goo-
dc.citation.volume53-
dc.citation.number1-
dc.citation.startPage75-
dc.citation.endPage81-
dc.identifier.bibliographicCitationJournal of Clinical Pharmacology, Vol.53(1) : 75-81, 2013-
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Pharmacology (약리학교실) > 1. Journal Papers

qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.