Principles of early drug discovery

Br J Pharmacol. 2011 Mar;162(6):1239-49. doi: 10.1111/j.1476-5381.2010.01127.x.


Developing a new drug from original idea to the launch of a finished product is a complex process which can take 12-15 years and cost in excess of $1 billion. The idea for a target can come from a variety of sources including academic and clinical research and from the commercial sector. It may take many years to build up a body of supporting evidence before selecting a target for a costly drug discovery programme. Once a target has been chosen, the pharmaceutical industry and more recently some academic centres have streamlined a number of early processes to identify molecules which possess suitable characteristics to make acceptable drugs. This review will look at key preclinical stages of the drug discovery process, from initial target identification and validation, through assay development, high throughput screening, hit identification, lead optimization and finally the selection of a candidate molecule for clinical development.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Drug Design
  • Drug Discovery*
  • Drug Evaluation, Preclinical
  • Drug Industry*
  • High-Throughput Screening Assays*
  • Humans
  • Molecular Targeted Therapy*