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In Vitro DDI Assessments


    🔔 Note: Stop playback at 40:20 to complete this lesson.


    Presenter

    Xinning Yang, PhD
    Policy Lead
    Guidance & Policy Team
    Office of Clinical Pharmacology (OCP)
    Office of Translational Sciences (OTS)
    Center for Drug Evaluation and Research (CDER)
    US Food and Drug Administration (FDA)

    Abstract

    This presentation details in vitro drug-drug interaction (DDI) assessments as outlined in the new ICH M12 guideline, contrasting it with previous FDA guidance. It emphasizes the importance of conducting these evaluations early in drug development to guide clinical study needs and protocol decisions. The speaker covers assessing investigational drugs as substrates, inhibitors, or inducers of CYP enzymes and drug transporters. Key updates include increased flexibility for plasma protein binding determination, refined criteria for CYP inhibition and induction (e.g., new scaling factors for time-dependent inhibitors and inducers), and revised cutoff values for transporter inhibition. The presentation also addresses the DDI liability of metabolites, detailing when their inhibition or induction potential requires evaluation, especially for major metabolites. Lastly, it discusses UGT-mediated DDIs, noting the challenges in predicting their in vivo potential from in vitro data and the limited clinical significance often observed. The speaker highlights areas warranting further research to enhance the efficiency and accuracy of DDI assessments.

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