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2018 (v.26 no.3)

Translational and Clinical Pharmacology

Korean Society for Clinical Pharmacology and Therapeutics
ISSN: 2289-0882

  • Mechanistic ligand-receptor interaction model: operational model of agonism

    Hyungsub Kim, Hyeong-Seok Lim

    TCP | v.26, no.3, pp.115-117, Sep, 2018


    This tutorial explains the basic principles of mechanistic ligand-receptor interaction model, which
    is an operational model of agonism. A growing number of agonist drugs, especially immune oncology
    drugs, is currently being developed. In this tutorial, time-dependent ordinary differential
    equation for simple Emax operational model of agonism was derived step by step. The differential
    equation could be applied in a pharmacodynamic modeling software, such as NONMEM, for use
    in non-steady state experiments, in which experimental data are generated while the interaction between
    ligand and receptor changes over time. Making the most of the non-steady state experimental
    data would simplify the experimental processes, and furthermore allow us to identify more detailed
    kinetics of a potential drug. The operational model of agonism could be useful to predict the optimal
    dose for agonistic drugs from in vitro and in vivo animal pharmacology experiments at the very
    early phase of drug development.


    Mechanistic ligand-receptor interaction, Operational model of agonism, Optimal dose, Prediction