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Effect of Itraconazole, a Potent CYP3A4 Inhibitor, on the Steady-State Pharmacokinetics of Vemurafenib in Patients With BRAFV600 Mutation-Positive Malignancies

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dc.contributor.author신상준-
dc.date.accessioned2022-11-24T00:55:00Z-
dc.date.available2022-11-24T00:55:00Z-
dc.date.issued2021-01-
dc.identifier.issn2160-763X-
dc.identifier.urihttps://ir.ymlib.yonsei.ac.kr/handle/22282913/191077-
dc.description.abstractThe effects of itraconazole, a strong CYP3A4 inhibitor, on the steady-state pharmacokinetics of vemurafenib were evaluated in a phase 1, multicenter, open-label, fixed-sequence study. Patients with BRAFV600 mutation-positive metastatic malignancies received oral vemurafenib 960 mg twice daily on days 1 to 20 (period A) and oral vemurafenib 960 mg twice daily with oral itraconazole 200 mg once daily on days 21 to 40 (period B). A mixed-effects analysis of variance model was used to compare log-transformed area under the concentration-time curve during the dosing interval and maximum plasma concentration values for vemurafenib in 8 patients between period B (vemurafenib plus itraconazole) and period A (vemurafenib alone). Multiple doses of itraconazole increased steady-state exposure of vemurafenib by approximately 40%, with geometric least squares mean ratios (period B/period A) of 140% (90% confidence interval, 121-161) for both maximum plasma concentration and area under the concentration-time curve during the dosing interval. There was no apparent increase in incidence or severity of adverse events during coadministration of vemurafenib with itraconazole. In conclusion, coadministration of itraconazole with vemurafenib resulted in a modest increase in exposure of vemurafenib at steady state and was generally well tolerated.-
dc.description.statementOfResponsibilityrestriction-
dc.languageEnglish-
dc.publisherWiley-
dc.relation.isPartOfCLINICAL PHARMACOLOGY IN DRUG DEVELOPMENT-
dc.rightsCC BY-NC-ND 2.0 KR-
dc.subject.MESHAdult-
dc.subject.MESHAged-
dc.subject.MESHAged, 80 and over-
dc.subject.MESHAntineoplastic Agents / administration & dosage-
dc.subject.MESHAntineoplastic Agents / adverse effects-
dc.subject.MESHAntineoplastic Agents / blood-
dc.subject.MESHAntineoplastic Agents / pharmacokinetics*-
dc.subject.MESHCytochrome P-450 CYP3A Inhibitors / administration & dosage*-
dc.subject.MESHCytochrome P-450 CYP3A Inhibitors / adverse effects-
dc.subject.MESHDrug Interactions-
dc.subject.MESHFemale-
dc.subject.MESHHumans-
dc.subject.MESHItraconazole / administration & dosage*-
dc.subject.MESHItraconazole / adverse effects-
dc.subject.MESHMale-
dc.subject.MESHMelanoma / blood-
dc.subject.MESHMelanoma / drug therapy-
dc.subject.MESHMelanoma / genetics-
dc.subject.MESHMelanoma / metabolism*-
dc.subject.MESHMiddle Aged-
dc.subject.MESHMutation-
dc.subject.MESHProtein Kinase Inhibitors / administration & dosage-
dc.subject.MESHProtein Kinase Inhibitors / adverse effects-
dc.subject.MESHProtein Kinase Inhibitors / blood-
dc.subject.MESHProtein Kinase Inhibitors / pharmacokinetics*-
dc.subject.MESHProto-Oncogene Proteins B-raf / genetics-
dc.subject.MESHThyroid Neoplasms / blood-
dc.subject.MESHThyroid Neoplasms / drug therapy-
dc.subject.MESHThyroid Neoplasms / genetics-
dc.subject.MESHThyroid Neoplasms / metabolism*-
dc.subject.MESHVemurafenib / administration & dosage-
dc.subject.MESHVemurafenib / adverse effects-
dc.subject.MESHVemurafenib / blood-
dc.subject.MESHVemurafenib / pharmacokinetics*-
dc.subject.MESHYoung Adult-
dc.titleEffect of Itraconazole, a Potent CYP3A4 Inhibitor, on the Steady-State Pharmacokinetics of Vemurafenib in Patients With BRAFV600 Mutation-Positive Malignancies-
dc.typeArticle-
dc.contributor.collegeCollege of Medicine (의과대학)-
dc.contributor.departmentDept. of Internal Medicine (내과학교실)-
dc.contributor.googleauthorWeijiang Zhang-
dc.contributor.googleauthorMichael Mathisen-
dc.contributor.googleauthorGrant R Goodman-
dc.contributor.googleauthorHarper Forbes-
dc.contributor.googleauthorYuyao Song-
dc.contributor.googleauthorEnric Bertran-
dc.contributor.googleauthorLev Demidov-
dc.contributor.googleauthorSang Joon Shin-
dc.identifier.doi10.1002/cpdd.822-
dc.contributor.localIdA02105-
dc.relation.journalcodeJ04263-
dc.identifier.eissn2160-7648-
dc.identifier.pmid32602215-
dc.identifier.urlhttps://accp1.onlinelibrary.wiley.com/doi/10.1002/cpdd.822-
dc.subject.keywordCYP3A4-
dc.subject.keyworddrug-drug interactions-
dc.subject.keyworditraconazole-
dc.subject.keywordpharmacokinetics-
dc.subject.keywordvemurafenib-
dc.contributor.alternativeNameShin, Sang Joon-
dc.contributor.affiliatedAuthor신상준-
dc.citation.volume10-
dc.citation.number1-
dc.citation.startPage39-
dc.citation.endPage45-
dc.identifier.bibliographicCitationCLINICAL PHARMACOLOGY IN DRUG DEVELOPMENT, Vol.10(1) : 39-45, 2021-01-
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Internal Medicine (내과학교실) > 1. Journal Papers

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