Kinase drug discovery 20 years after imatinib: progress and future directions

Philip Cohen (Lead / Corresponding author), Darren Cross (Lead / Corresponding author), Pasi A. Jänne (Lead / Corresponding author)

Research output: Contribution to journalReview articlepeer-review

498 Citations (Scopus)


Protein kinases regulate nearly all aspects of cell life, and alterations in their expression, or mutations in their genes, cause cancer and other diseases. Here, we review the remarkable progress made over the past 20 years in improving the potency and specificity of small-molecule inhibitors of protein and lipid kinases, resulting in the approval of more than 70 new drugs since imatinib was approved in 2001. These compounds have had a significant impact on the way in which we now treat cancers and non-cancerous conditions. We discuss how the challenge of drug resistance to kinase inhibitors is being met and the future of kinase drug discovery.

Original languageEnglish
Pages (from-to)551-569
Number of pages19
JournalNature Reviews Drug Discovery
Early online date17 May 2021
Publication statusPublished - Jul 2021


  • Drug discovery
  • Drug development
  • Small molecules

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology


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