2. Academic Validation
  3. HPLC-MS/MS analysis of mesupron and its application to a pharmacokinetic study in rats

HPLC-MS/MS analysis of mesupron and its application to a pharmacokinetic study in rats

  • J Pharm Biomed Anal. 2018 Feb 20;150:39-42. doi: 10.1016/j.jpba.2017.12.002.
Changmin Park 1,  Joong Gyu Ha 2,  Seungmok Choi 1,  Eunyoung Kim 1,  Keumhan Noh 3,  Beom Soo Shin 4,  Wonku Kang 5
Affiliations

Affiliations

  • 1 College of Pharmacy, Chung-Ang University, Seoul 06974, South Korea.
  • 2 Department of Obstetrics and Gynecology, Eulji University Hospital, Eulji University School of Medicine, Daejeon 35233, South Korea.
  • 3 Department of Pharmaceutical Sciences, Leslie Dan Faculty of Pharmacy, University of Toronto, 144 College Street, Toronto, Canada.
  • 4 School of Pharmacy, Sungkyunkwan University, Gyeonggi-do 16419, South Korea. Electronic address: bsshin@skku.edu.
  • 5 College of Pharmacy, Chung-Ang University, Seoul 06974, South Korea. Electronic address: wkang@cau.ac.kr.
PMID: 29216583 DOI: 10.1016/j.jpba.2017.12.002
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.

Keywords

LC–MS/MS; Mesupron; Pharmacokinetics; Rat.

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