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Simultaneous determination of the novel thiosemicarbazone anti-cancer agent, Bp4eT, and its main phase I metabolites in plasma: Application to a pilot pharmacokinetic study in rats

Publication at Faculty of Pharmacy in Hradec Králové |
2014

Abstract

This study describes the first validated LC-MS/MS method for the simultaneous quantification of 2-benzoylpyridine 4-ethyl-3-thiosemicarbazone (Bp4eT) and its main metabolites (E/Z isomers of the semicarbazone structure, M1-E and M1-Z, and the amidrazone metabolite, M2) in plasma. This method was validated over the concentration range of 0.18-2.80 microM for Bp4eT, 0.02-0.37 microM for both M1-E and M1-Z, and 0.10-1.60 microM for M2.

This methodology was applied to the analysis of samples from in vivo experiments, allowing for the concentration-time profile to be simultaneously assessed for the parent drug and its metabolites.