Academic Journal
Evaluation of the inhibitory effect of azoles on pharmacokinetics of lenvatinib in rats both in vivo and in vitro by UPLC‐MS/MS
| العنوان: | Evaluation of the inhibitory effect of azoles on pharmacokinetics of lenvatinib in rats both in vivo and in vitro by UPLC‐MS/MS |
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| المؤلفون: | Mengming Xia, Xueyi Song, Zebei Lu, Yu Wang, Quan Zhou, Peiwu Geng, Shuanghu Wang, Yunfang Zhou, Qingjun Wu, Aixia Han |
| المصدر: | Thoracic Cancer, Vol 14, Iss 33, Pp 3331-3341 (2023) |
| بيانات النشر: | Wiley, 2023. |
| سنة النشر: | 2023 |
| المجموعة: | LCC:Neoplasms. Tumors. Oncology. Including cancer and carcinogens |
| مصطلحات موضوعية: | azoles, CYP3A4, drug‐drug interactions, lenvatinib, pharmacokinetic, Neoplasms. Tumors. Oncology. Including cancer and carcinogens, RC254-282 |
| الوصف: | Abstract Background Lenvatinib is a multitargeted tyrosine kinase inhibitor used in the treatment of a variety of solid tumors. This study aims to investigate the potential pharmacokinetic interactions between lenvatinib and various azoles (ketoconazole, voriconazole, isavuconazole and posaconazole) when orally administered to rats. Methods A total of 30 Sprague–Dawley rats were randomly allocated into five groups and administered 20 mg/kg of ketoconazole, voriconazole, isavuconazole and 30 mg/kg of posaconazole and 0.5% CMC‐Na, through gavage for a duration of 7 days prior to the commencement of the experiment. On the final day, the rats were given 10 mg/kg of lenvatinib. The blood concentration of lenvatinib was determined using UPLC‐MS–MS. In vitro lenvatinib were incubated with azoles and rat liver microsomes (RLMs) or human liver microsomes (HLMs). Molecular docking was lastly used to examine the binding strength of the enzymes and ligands with Autodock Vina. Results AUC and Cmax of lenvatinib significantly increased with each of the azoles (p |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 1759-7714 1759-7706 |
| Relation: | https://doaj.org/toc/1759-7706; https://doaj.org/toc/1759-7714 |
| DOI: | 10.1111/1759-7714.15125 |
| URL الوصول: | https://doaj.org/article/4d7266ab9388414f9cac2b1337c25198 |
| رقم الانضمام: | edsdoj.4d7266ab9388414f9cac2b1337c25198 |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 17597714 17597706 |
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| DOI: | 10.1111/1759-7714.15125 |