Cited 3 times in
Effect of Vemurafenib on the Pharmacokinetics of a Single Dose of Tizanidine (a CYP1A2 Substrate) in Patients With BRAF V600 Mutation-Positive Malignancies
DC Field | Value | Language |
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dc.contributor.author | 최혜진 | - |
dc.date.accessioned | 2022-09-02T01:12:56Z | - |
dc.date.available | 2022-09-02T01:12:56Z | - |
dc.date.issued | 2020-07 | - |
dc.identifier.issn | 2160-763X | - |
dc.identifier.uri | https://ir.ymlib.yonsei.ac.kr/handle/22282913/190064 | - |
dc.description.abstract | This phase 1 open-label, multicenter, 3-period, fixed-sequence study evaluated the effect of multiple doses of vemurafenib on the pharmacokinetics of 1 dose of tizanidine, a probe CYP1A2 substrate, in patients with BRAF(V600) mutation-positive metastatic malignancy. Patients received 1 dose of tizanidine 2 mg on day 1 (period A), vemurafenib 960 mg twice daily on days 2-21 (period B), and 1 dose of tizanidine 2 mg and vemurafenib 960 mg twice daily on day 22 (period C). Log-transformed area under the concentration-time curve (AUC) and maximum plasma concentration (C-max) values for tizanidine in 16 patients were compared between periods A (tizanidine alone) and C (tizanidine plus vemurafenib) using an analysis of variance model. Multiple doses of vemurafenib increased plasma exposure of 1 dose of tizanidine, with geometric mean ratios (period C/period A) for C-max, AUC(inf), and AUC(last) of 2.15 (90%CI, 1.71-2.71), 4.22 (90%CI, 3.37-5.28), and 4.74 (90%CI, 3.55-6.33), respectively; 90%CIs were all outside predefined limits for lack of drug-drug interaction (0.82-1.22). This study confirmed vemurafenib as a moderate inhibitor of CYP1A2 in vivo, with a statistically significant drug-drug interaction with tizanidine. Caution should be exercised when dosing vemurafenib concurrently with CYP1A2 substrates. | - |
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 | Clonidine / administration & dosage | - |
dc.subject.MESH | Clonidine / analogs & derivatives* | - |
dc.subject.MESH | Clonidine / blood | - |
dc.subject.MESH | Clonidine / pharmacokinetics | - |
dc.subject.MESH | Cyprus / epidemiology | - |
dc.subject.MESH | Cytochrome P-450 CYP1A2 / drug effects* | - |
dc.subject.MESH | Drug Interactions | - |
dc.subject.MESH | Female | - |
dc.subject.MESH | Humans | - |
dc.subject.MESH | Male | - |
dc.subject.MESH | Middle Aged | - |
dc.subject.MESH | Mutation | - |
dc.subject.MESH | Neoplasm Metastasis / drug therapy* | - |
dc.subject.MESH | Neoplasm Metastasis / genetics | - |
dc.subject.MESH | Neoplasm Metastasis / pathology | - |
dc.subject.MESH | Neoplasm Staging | - |
dc.subject.MESH | Neoplasms / blood | - |
dc.subject.MESH | Neoplasms / drug therapy* | - |
dc.subject.MESH | Neoplasms / genetics | - |
dc.subject.MESH | Neoplasms / pathology | - |
dc.subject.MESH | Parasympatholytics / administration & dosage | - |
dc.subject.MESH | Parasympatholytics / blood | - |
dc.subject.MESH | Parasympatholytics / pharmacokinetics | - |
dc.subject.MESH | Protein Kinase Inhibitors / administration & dosage | - |
dc.subject.MESH | Protein Kinase Inhibitors / adverse effects* | - |
dc.subject.MESH | Protein Kinase Inhibitors / pharmacokinetics | - |
dc.subject.MESH | Proto-Oncogene Proteins B-raf / drug effects | - |
dc.subject.MESH | Proto-Oncogene Proteins B-raf / genetics | - |
dc.subject.MESH | Proto-Oncogene Proteins B-raf / metabolism | - |
dc.subject.MESH | Republic of Korea / epidemiology | - |
dc.subject.MESH | Vemurafenib / administration & dosage | - |
dc.subject.MESH | Vemurafenib / adverse effects | - |
dc.subject.MESH | Vemurafenib / pharmacokinetics* | - |
dc.title | Effect of Vemurafenib on the Pharmacokinetics of a Single Dose of Tizanidine (a CYP1A2 Substrate) in Patients With BRAF V600 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 | Christine McIntyre | - |
dc.contributor.googleauthor | Todd Riehl | - |
dc.contributor.googleauthor | Harper Forbes | - |
dc.contributor.googleauthor | Enric Bertran | - |
dc.contributor.googleauthor | Hye Jin Choi | - |
dc.contributor.googleauthor | Dae Ho Lee | - |
dc.contributor.googleauthor | Jeeyun Lee | - |
dc.identifier.doi | 10.1002/cpdd.788 | - |
dc.contributor.localId | A04219 | - |
dc.relation.journalcode | J04263 | - |
dc.identifier.eissn | 2160-7648 | - |
dc.identifier.pmid | 32311241 | - |
dc.identifier.url | https://accp1.onlinelibrary.wiley.com/doi/10.1002/cpdd.788 | - |
dc.subject.keyword | drug-drug interactions | - |
dc.subject.keyword | pharmacokinetics | - |
dc.subject.keyword | tizanidine | - |
dc.subject.keyword | vemurafenib | - |
dc.contributor.alternativeName | Choi, Hye Jin | - |
dc.contributor.affiliatedAuthor | 최혜진 | - |
dc.citation.volume | 9 | - |
dc.citation.number | 5 | - |
dc.citation.startPage | 651 | - |
dc.citation.endPage | 658 | - |
dc.identifier.bibliographicCitation | CLINICAL PHARMACOLOGY IN DRUG DEVELOPMENT, Vol.9(5) : 651-658, 2020-07 | - |
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