Industries: Pharma / Biotech

Developability Assessment – The Logical Approach to Discovery Lead Selection

Course Director: Duane B. Lakings, Ph.D.

Course Fee: $2150.00 Regular Registration / $1950.00 Early Bird (30 Days in Advance)

 

Lead Discovery Training

Course Description - Course runs 9:00 - 5:00 on Day 1 & Day 2 

The content of this course will assist pharmaceutical, biotechnology, and CRO researchers and managers in understanding the requirements for a logical, well designed, and successful developability assessment or discovery lead optimization program. The various types of experiments, which include in vitro and in vivo pharmacology, stability and solubility assessments, in vitro drug metabolism and delivery, preliminary animal pharmacokinetics, and in vitro and acute toxicology, will be described and discussed. Study designs and potential results, with possible interpretations, from each of the study types will be presented.

Examples of developability assessment logic plans for various types of drug discovery programs will be presented and a workshop will provide participants with the opportunity to design and discuss other logic plan types.

Who Should Attend

This two-day course is specifically designed for personnel in the pharmaceutical and biotechnology industries and contract research organizations (CROs) who are involved in drug discovery and early drug development and who want to have a better understanding of the approaches and techniques available for discovery lead selection and optimization. Participants should have some knowledge of drug discovery and development and desire to learn more about how to logically design, conduct, and interpret lead optimization experiments in order the select the optimal compound for preclinical development. 

Drug discovery and development scientists, managers, and project team leaders at pharmaceutical companies and related industries will gain a detailed understanding of the types of developability assessment research studies that can be conducted to determine the drug-like attributes and potential demerits of a discovery lead or group of leads.

Course Agenda

DAY ONE

Session 1: Introduction and Overview (8:30 – 10:00 AM)

  • Purpose and Goals
  • Drug Discovery and Development Logic Plan
  • Review of Drug Discovery
  • Where Developability Assessment Fits Into the Logic Plan
  • Overview of Developability Assessment Scientific Disciplines

Session 2: In Vitro and In Vivo Pharmacology (10:30 AM to noon)

  • In Vitro Pharmacology
  • Expansion of Drug Discovery Results
  • 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 Study Design
  • Example In Vivo Dose Response Curves

Session 3: Early Formulation Evaluations (1:00 PM to 2:30 PM)

  • Analytical Chemistry Method Development and Characterization
  • Stability and Solubility Requirements
  • Example Stability and Solubility Profiles

Session 4: In Vitro Drug Delivery and Metabolism (3:00 PM to 4:30 PM)

  • In Vitro Delivery
  • GI Tract
  • Blood Brain Barrier
  • Skin and Other Member Types
  • Example Delivery Profiles
  • In Vitro Metabolism
  • Preliminary Protein Binding
  • P-450 Isozymes, Microsomes, and/or Hepatocytes
  • Phase II Metabolism
  • Species-Species Comparisons
  • Example Metabolism Profiles

DAY TWO

Session 5: Preliminary Animal Pharmacokinetics (8:30 AM to 10:00 AM)

  • Bioanalytical Chemistry Method Development and Characterization
  • Stereospecific and Pro-drug Bioanalytical Chemistry Method Requirements
  • Pharmacokinetic Experiments and Example Profiles
  • Bioavailability Assessments and Example Profiles

Session 6:  Bioavailability Assessments and Example Profiles (10:30 AM to noon)

  • In Vitro Toxicology
  • Acute or Single-Dose Toxicology
  • Safety Pharmacology
  • Genotoxicity

Session 7: Developability Assessment Logic Plan Generation Examples (1:00 PM to 2:30 PM)

  • Life-threatening Disorder with Acute Intravenous Dosing
  • Non-life-threatening Disorder with Chronic Oral Dosing

Session 8: Workshop to Design and Discuss Participant Prepared Developability Assessment Logic Plans (3:00 PM to 4:30 PM)

© Course Description and Agenda 2019 CfPIE, Inc. All Rights Reserved

Learning Objectives

Upon completing this course, participants will have gained the knowledge to design a logic plan of in vitro and in vivo research studies needed to evaluate the attributes and potential demerits of drug discovery leads, either small organic molecules (NCEs) or macromolecules. Participants will learn about and understand the requirements for selecting a discovery lead with a better chance of successfully completing the preclinical development effort needed to support first-in-human clinical trials.

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