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A practical view of 'druggability'.

Thomas H Keller1, Arkadius Pichota, Zheng Yin

  • 1Novartis Institute for Tropical Diseases, 10 Biopolis Road, #05-01 Chromos, 138670 Singapore. thomas.keller@novartis.com

Current Opinion in Chemical Biology
|July 4, 2006
PubMed
Summary

Lipinski's Rule of Five revolutionized drug discovery by emphasizing pharmacokinetic properties. Medicinal chemists now integrate drug-likeness and druggability early for successful lead optimization.

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Area of Science:

  • Medicinal Chemistry
  • Pharmacokinetics
  • Drug Discovery

Background:

  • Lipinski's Rule of Five significantly altered medicinal chemists' approach to drug design.
  • Early consideration of pharmacokinetic properties became crucial during lead optimization.
  • Concepts of drug-likeness and druggability expanded to target identification (proteins and genes).

Purpose of the Study:

  • To review recent advancements in applying drug-likeness and druggability concepts.
  • To examine the practical utility of these 'rules of the game' for medicinal chemists.
  • To provide a medicinal chemist's perspective on integrating these principles into drug discovery.

Main Methods:

  • Literature review of recent advances in drug discovery and optimization.
  • Analysis of the practical application of drug-likeness and druggability rules.
  • Synthesis of a medicinal chemist's viewpoint on current methodologies.

Main Results:

  • The Rule of Five has fundamentally shifted the focus in drug discovery towards pharmacokinetics.
  • Drug-likeness and druggability are now integral considerations from target identification to lead optimization.
  • Practical integration of these concepts remains an active area of development and refinement.

Conclusions:

  • The principles derived from Lipinski's Rule of Five are essential for modern drug discovery.
  • Medicinal chemists must continuously adapt and integrate these evolving concepts for efficient drug development.
  • Further examination of practical implementation is needed to maximize the benefits of drug-likeness and druggability criteria.

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