For the quantitative estimation of the therapeutic/pharmacological effects and adverse/toxic reactions of drugs act on a specific receptor, we developed an integrated pharmacokinetic system incorporat ing pharmacokinetics, receptor occupancy theory and a ternary complex model. The developed system ena bled to predict the optimal dosage for an investigational drug by using pre-clinical and clinical data (phase I study) under development, and to assess quantitatively the intensity of its

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... oxic reactions, which may not be detectable in the trial stage. As for commercially available drug, the developed system may be useful to provide the optimal dosage regimen, which offers the desired therapeutic effects with minimum ad verse/toxic effects. This methodology may be applied for the evaluation of the therapeutic and/or adverse effects of drugs with other mechanisms of action, such as an enzyme inhibitors/inducers, in future.