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2020•BioanalysisRequires access

A UHPLC–MS/MS Method to Determine FLZ Major Active Metabolites in Human Plasma: Application to a Pharmacokinetic Study

Teng Wang, Huanhuan Wang, Rui Chen, Ji Jiang, Qian Zhao, Pei Hu

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Abstract

Aim: FLZ, a novel promising dopamine neuroprotective agent, is designed to treat Parkinson's disease. F7G and F21G are FLZ major active Phase II metabolites whose exposure are nearly 100-times higher than FLZ, may chiefly produce effectiveness in human. Measurement of F7G and F21G in plasma samples is critical for investigating its pharmacokinetics in clinical studies. Methodology & results: Plasma samples were extracted by SPE method and then analyzed by a newly established ultra-UHPLC–MS/MS method. Conclusion: For the first time, a reliable and robust bioanalytical method for F7G and F21G detection was successfully applied in a first-in-human study.

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What this paper is about

Aim: FLZ, a novel promising dopamine neuroprotective agent, is designed to treat Parkinson's disease. F7G and F21G are FLZ major active Phase II metabolites whose exposure are nearly 100-times higher than FLZ, may chiefly produce effectiveness in human. Measurement of F7G and F21G in plasma samples is critical for investigating its pharmacokinetics in clinical studies. Methodology & results: Plasma samples were extracted by SPE method and then analyzed by a newly established ultra-UHPLC–MS/MS method. Conclusion: For the first time, a reliable and robust bioanalytical method for F7G and F21G detection was successfully applied in a first-in-human study.

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Available abstract

Aim: FLZ, a novel promising dopamine neuroprotective agent, is designed to treat Parkinson's disease. F7G and F21G are FLZ major active Phase II metabolites whose exposure are nearly 100-times higher than FLZ, may chiefly produce effectiveness in human. Measurement of F7G and F21G in plasma samples is critical for investigating its pharmacokinetics in clinical studies. Methodology & results: Plasma samples were extracted by SPE method and then analyzed by a newly established ultra-UHPLC–MS/MS method. Conclusion: For the first time, a reliable and robust bioanalytical method for F7G and F21G detection was successfully applied in a first-in-human study.

Key concepts: Pharmacokinetics, Active metabolite, Human plasma, Chemistry, Chromatography, Bioanalysis, Metabolite, Plasma concentration

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