Overview of Drug Discovery and Development

Mark A. Ator1, John P. Mallamo1, Michael Williams1

1 Cephalon, Inc., West Chester, Pennsylvania
Publication Name:  Current Protocols in Pharmacology
Unit Number:  Unit 9.9
DOI:  10.1002/0471141755.ph0909s35
Online Posting Date:  December, 2006
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This overview unit describes the core activities involved in the drug discovery and development process, from target identification ‐ including preclinical biology, medicinal and process chemistry ‐ to pharmacokinetics and metabolism (ADME), and also activities related to the to the drug approval process. The latter include the activities related to the filing of an IND (Investigational New Drug) application and also Phases I – III of clinical trials that form the basis of an NDA (New Drug Application) submission, as well as post‐marketing Phase IV activities as required by the U.S. Food and Drug Administration (FDA) and the European and Japanese counterparts

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Table of Contents

  • Introduction
  • Pharmacology
  • Medicinal Chemistry
  • Drug Discovery
  • Drug Targets
  • Lead Discovery
  • Compound Sources
  • Biologicals, Antisense, and RNA Interference
  • Computational Chemistry
  • High‐Throughput Screening
  • Hit to Lead
  • Lead Optimization
  • Structure‐Activity Relationships (SARs)
  • Drug Metabolism and Pharmacokinetics
  • Preclinical Development
  • Literature Cited
  • Figures
  • Tables
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Literature Cited

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