HPLC-MS/MS analysis of mesupron and its application to a pharmacokinetic study in rats
- Authors
- Park, Changmin; Ha, Joong Gyu; Choi, Seungmok; Kim, Eunyoung; Noh, Keumhari; Shin, Beom Soo; Kang, Wonku
- Issue Date
- Feb-2018
- Publisher
- ELSEVIER SCIENCE BV
- Keywords
- Mesupron; LC-MS/MS; Rat; Pharmacokinetics
- Citation
- JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, v.150, pp 39 - 42
- Pages
- 4
- Journal Title
- JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
- Volume
- 150
- Start Page
- 39
- End Page
- 42
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/1184
- DOI
- 10.1016/j.jpba.2017.12.002
- ISSN
- 0731-7085
1873-264X
- Abstract
- Mesupron, the first-in-class inhibitor of urokinase-type plasminogen activator (uPA) is known to regulate cell proliferation and migration, and is under investigation for the treatment of metastatic breast cancer. In this study, a quantification method was developed for the determination of mesupron in rat plasma using liquid chromatography with a tandem mass spectrometry (LC-MS/MS). After protein precipitation with acetonitrile including itraconazole (internal standard, IS), the analytes were chromatographed on a reversed phased column with a mobile phase of acetonitrile and water (7:3, v/v, including 0.1% formic acid). The ion transitions of the precursor to the product ion were principally protonated ion [M+H](+) at m/z 630.4 -> 398.3 for mesupron and 705.2 -> 392.1 for the IS. The accuracy and precision of the assay were in accordance with FDA regulations for the validation of bioanalytical methods This method was successfully applied to a pharmacokinetic study of mesupron after intravenous administration in rats. (C) 2017 Elsevier B.V. All rights reserved.
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