An Accessible Pharmacodynamic Transcriptional Biomarker for Notch Target Engagement

    February 2016 in “ Clinical Pharmacology & Therapeutics ”
    Keith Q. Tanis, Alexei A. Podtelezhnikov, Samuel C. Blackman, Jeremy Hing, Radha Railkar, Jared Lunceford, Joel A. Klappenbach, Bo Wei, Amy Harman, Luiz Miguel Camargo, Sanjiv Shah, Eva M. Finney, James S. Hardwick, Andrey Loboda, James Watters, Donald A. Bergstrom, Tim Demuth, Gary Herman, Peter R. Strack, Robert Iannone
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    TLDR Hair follicle samples effectively show how well the drug MK-0752 targets and engages with the Notch pathway.
    The document reports on a clinical trial that investigated the effects of the gamma-secretase inhibitor MK-0752 on gene expression related to the Notch signaling pathway. The trial included 24 subjects who were given MK-0752 or a placebo, and their blood and hair follicle samples were analyzed for changes in a predefined 11-gene Notch signature. The study found that hair follicle samples were more reliable than blood samples for analysis, with 430 hair follicle samples passing quality control compared to 119 blood samples. The Notch signature score in hair follicles was identified as a reliable biomarker for MK-0752 target engagement, and the drug was found to be well-tolerated. The study was funded by Merck & Co., Inc., and the authors disclosed their employment and stock ownership in the company.
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