A decade of fragment-based drug design: strategic advances and lessons learned

Nat Rev Drug Discov. 2007 Mar;6(3):211-9. doi: 10.1038/nrd2220. Epub 2007 Feb 9.


Since the early 1990s, several technological and scientific advances - such as combinatorial chemistry, high-throughput screening and the sequencing of the human genome - have been heralded as remedies to the problems facing the pharmaceutical industry. The use of these technologies in some form is now well established at most pharmaceutical companies; however, the return on investment in terms of marketed products has not met expectations. Fragment-based drug design is another tool for drug discovery that has emerged in the past decade. Here, we describe the development and evolution of fragment-based drug design, analyse the role that this approach can have in combination with other discovery technologies and highlight the impact that fragment-based methods have made in progressing new medicines into the clinic.

Publication types

  • Review

MeSH terms

  • Decision Making, Organizational
  • Drug Design*
  • Drug Industry / organization & administration
  • Drug Industry / trends
  • Ligands
  • Molecular Structure
  • Technology, Pharmaceutical / methods*
  • Technology, Pharmaceutical / trends
  • Time Factors


  • Ligands