Cited 3 times in
Effect of Itraconazole, a Potent CYP3A4 Inhibitor, on the Steady-State Pharmacokinetics of Vemurafenib in Patients With BRAFV600 Mutation-Positive Malignancies
DC Field | Value | Language |
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dc.contributor.author | 신상준 | - |
dc.date.accessioned | 2022-11-24T00:55:00Z | - |
dc.date.available | 2022-11-24T00:55:00Z | - |
dc.date.issued | 2021-01 | - |
dc.identifier.issn | 2160-763X | - |
dc.identifier.uri | https://ir.ymlib.yonsei.ac.kr/handle/22282913/191077 | - |
dc.description.abstract | The 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.statementOfResponsibility | restriction | - |
dc.language | English | - |
dc.publisher | Wiley | - |
dc.relation.isPartOf | CLINICAL PHARMACOLOGY IN DRUG DEVELOPMENT | - |
dc.rights | CC BY-NC-ND 2.0 KR | - |
dc.subject.MESH | Adult | - |
dc.subject.MESH | Aged | - |
dc.subject.MESH | Aged, 80 and over | - |
dc.subject.MESH | Antineoplastic Agents / administration & dosage | - |
dc.subject.MESH | Antineoplastic Agents / adverse effects | - |
dc.subject.MESH | Antineoplastic Agents / blood | - |
dc.subject.MESH | Antineoplastic Agents / pharmacokinetics* | - |
dc.subject.MESH | Cytochrome P-450 CYP3A Inhibitors / administration & dosage* | - |
dc.subject.MESH | Cytochrome P-450 CYP3A Inhibitors / adverse effects | - |
dc.subject.MESH | Drug Interactions | - |
dc.subject.MESH | Female | - |
dc.subject.MESH | Humans | - |
dc.subject.MESH | Itraconazole / administration & dosage* | - |
dc.subject.MESH | Itraconazole / adverse effects | - |
dc.subject.MESH | Male | - |
dc.subject.MESH | Melanoma / blood | - |
dc.subject.MESH | Melanoma / drug therapy | - |
dc.subject.MESH | Melanoma / genetics | - |
dc.subject.MESH | Melanoma / metabolism* | - |
dc.subject.MESH | Middle Aged | - |
dc.subject.MESH | Mutation | - |
dc.subject.MESH | Protein Kinase Inhibitors / administration & dosage | - |
dc.subject.MESH | Protein Kinase Inhibitors / adverse effects | - |
dc.subject.MESH | Protein Kinase Inhibitors / blood | - |
dc.subject.MESH | Protein Kinase Inhibitors / pharmacokinetics* | - |
dc.subject.MESH | Proto-Oncogene Proteins B-raf / genetics | - |
dc.subject.MESH | Thyroid Neoplasms / blood | - |
dc.subject.MESH | Thyroid Neoplasms / drug therapy | - |
dc.subject.MESH | Thyroid Neoplasms / genetics | - |
dc.subject.MESH | Thyroid Neoplasms / metabolism* | - |
dc.subject.MESH | Vemurafenib / administration & dosage | - |
dc.subject.MESH | Vemurafenib / adverse effects | - |
dc.subject.MESH | Vemurafenib / blood | - |
dc.subject.MESH | Vemurafenib / pharmacokinetics* | - |
dc.subject.MESH | Young Adult | - |
dc.title | Effect of Itraconazole, a Potent CYP3A4 Inhibitor, on the Steady-State Pharmacokinetics of Vemurafenib in Patients With BRAFV600 Mutation-Positive Malignancies | - |
dc.type | Article | - |
dc.contributor.college | College of Medicine (의과대학) | - |
dc.contributor.department | Dept. of Internal Medicine (내과학교실) | - |
dc.contributor.googleauthor | Weijiang Zhang | - |
dc.contributor.googleauthor | Michael Mathisen | - |
dc.contributor.googleauthor | Grant R Goodman | - |
dc.contributor.googleauthor | Harper Forbes | - |
dc.contributor.googleauthor | Yuyao Song | - |
dc.contributor.googleauthor | Enric Bertran | - |
dc.contributor.googleauthor | Lev Demidov | - |
dc.contributor.googleauthor | Sang Joon Shin | - |
dc.identifier.doi | 10.1002/cpdd.822 | - |
dc.contributor.localId | A02105 | - |
dc.relation.journalcode | J04263 | - |
dc.identifier.eissn | 2160-7648 | - |
dc.identifier.pmid | 32602215 | - |
dc.identifier.url | https://accp1.onlinelibrary.wiley.com/doi/10.1002/cpdd.822 | - |
dc.subject.keyword | CYP3A4 | - |
dc.subject.keyword | drug-drug interactions | - |
dc.subject.keyword | itraconazole | - |
dc.subject.keyword | pharmacokinetics | - |
dc.subject.keyword | vemurafenib | - |
dc.contributor.alternativeName | Shin, Sang Joon | - |
dc.contributor.affiliatedAuthor | 신상준 | - |
dc.citation.volume | 10 | - |
dc.citation.number | 1 | - |
dc.citation.startPage | 39 | - |
dc.citation.endPage | 45 | - |
dc.identifier.bibliographicCitation | CLINICAL PHARMACOLOGY IN DRUG DEVELOPMENT, Vol.10(1) : 39-45, 2021-01 | - |
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