Developability Assessment Short Course Overview

Introduction and Overview

•Purpose and Goals

•Drug Discovery and Development Logic Plan

•Where Developability Assessment Fits Into the Logic Plan

•Overview of Developability Assessment Scientific Disciplines

•Review of Drug Discovery

In Vitro and In Vivo Pharmacology

            •In Vitro Pharmacology

      > Expansion of Drug Discovery Results

      > Determination of IC50 and IC90 Values

      > Example In Vitro Dose Response Curves

            •    In Vivo Pharmacology

      > Definition and Characterization of Animal Models

      > Determination of ED50 and ED10 Values and Therapeutic Ratio

      > Example In Vivo Dose Response Curves

Early Formulation Evaluations

•Analytical Chemistry Method Development and Characterization

•Early Formulation Definition and Assessments

•Stability and Solubility Requirements

•Example Stability and Solubility Profiles

In Vitro Drug Metabolism and Delivery

            •In Vitro Metabolism

       > GYP450 Isozymes, Microsomes, and/or Hepatocytes

       > Phase II Metabolism

       > Species Comparisons

       > Example Metabolism Profiles

            •    In Vitro Delivery

       > GI Tract and Example Absorption Profiles

       > Blood Brain Barrier

       > Skin and Other Member Types

Preliminary Animal Pharmacokinetics

•Bioanalytical Chemistry Method Development and Characterization

•Preliminary Protein Binding

•Pharmacokinetic Experiments and Example Profiles

•Search for Metabolites in Plasma, Urine, Bile

Early Toxicology Assessments

•In Vitro Toxicology

•Acute or Single-Dose Toxicology

•Safety Pharmacology

•Genotoxicity

Developability Assessment Logic Plan Generation Examples

Workshop to Design and Discuss Participant Prepared Developability Assessment Logic Plans