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Determination of doravirine in human plasma using liquid–liquid extraction and HPLC–MS/MS

    Rajesh Desai

    *Author for correspondence: Tel.: +1 215 652 4224; Fax: +1 215 652 4524;

    E-mail Address: rajesh_desai@merck.com

    Department of Pharmacokinetics, Pharmacodynamics & Drug Metabolism, MRL, Merck & Co., Inc., West Point, PA 19486-0004, USA

    ,
    Brad Roadcap

    Department of Pharmacokinetics, Pharmacodynamics & Drug Metabolism, MRL, Merck & Co., Inc., West Point, PA 19486-0004, USA

    ,
    Dina Goykhman

    Department of Pharmacokinetics, Pharmacodynamics & Drug Metabolism, MRL, Merck & Co., Inc., West Point, PA 19486-0004, USA

    &
    Eric Woolf

    Department of Pharmacokinetics, Pharmacodynamics & Drug Metabolism, MRL, Merck & Co., Inc., West Point, PA 19486-0004, USA

    Published Online:https://doi.org/10.4155/bio-2019-0116

    Aim: A method to quantitate doravirine (MK-1439) in human plasma has been developed to support human clinical trials designed to evaluate the safety, pharmacokinetics and efficacy of the compound. Methodology & results: The analyte was extracted using liquid–liquid extraction, separated on a reverse phase HPLC column, and detected on an API-4000 mass spectrometer using a Turbo-Ion spray source in positive ionization mode coupled with multiple reaction monitoring mode was used for quantification. The dynamic range for the assay was 0.02–10 ng/ml using 100 μl of human plasma. Conclusion: The assay was found to be sensitive, selective and reproducible and applied to support the doravirine clinical development program.

    Papers of special note have been highlighted as: • of interest; •• of considerable interest

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