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HPLC–MS/MS analysis of mesupron and its application to a pharmacokinetic study in rats
Park, Changmin,Ha, Joong Gyu,Choi, Seungmok,Kim, Eunyoung,Noh, Keumhan,Shin, Beom Soo,Kang, Wonku Elsevier 2018 Journal of pharmaceutical and biomedical analysis Vol.150 No.-
<P><B>Abstract</B></P> <P>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]<SUP>+</SUP> at <I>m</I>/<I>z</I> 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.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Mesupron is the first-in-class inhibitor of urokinase-type plasminogen activator. </LI> <LI> Mesupron is under investigation for the treatment of metastatic breast cancer. </LI> <LI> A sensitive determination method of mesupron was developed using LC–MS/MS. </LI> <LI> This method was successfully applied to a pharmacokinetic study of mesupron after intravenous administration in rats. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>