154 pages 

Date published 
December 2007 

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Kinase Therapeutic Pipelines: An Assessment of Targets and Agents in Development

By Peter Norman, PhD, MBA 

Recent developments reflect the explosion in the number of kinase inhibitors that have entered clinical development in the past few years:


  • By the end of 2006 seven kinase inhibitors had reached the market, three in the period December 2005-December 2006.
  • Their collective sales exceeded $4 billion.
  • Three more kinase inhibitors have been approved in 2007.
  • In addition to ongoing studies of approved kinase inhibitors seeking line extensions, a further 11 are in Phase III studies.
  • More than 130 kinase inhibitors are reported to be in either Phase I or Phase II clinical development, with 47 reported to be in Phase II studies.

Protein kinases constitute a large family of proteins that is now firmly established as a major class of drug targets for the pharmaceutical industry. The sequencing of the human genome has led to the identification of 518 protein kinases encoded within it—the human kinome. This constitutes one of the largest and most druggable classes of targets for the pharmaceutical industry, with the number of kinases exceeding the number of G-protein coupled receptors in the human genome.

An essential report for industry professionals working in R&D, portfolio management, and kinase product management, Kinase Inhibitors Pipelines: An Assessment of Targets and Agents in Development reviews the considerable array of drug development efforts directed at kinases and:

  • Provides profiles of the activities of the major companies as well as the kinase inhibitors in development, and some of the specialist companies active in the field
  • Assesses the potential impact of the more advanced kinase inhibitors, which offer significant market potential
  • Discusses some of the technical challenges faced in developing such inhibitors
  • Concludes with commentaries from leading experts in the field


With so many inhibitors reported to be in clinical development and many more in preclinical development, kinase inhibitors now make up a significant fraction of most major pharmaceutical companies' pipelines, as well as an area of focus for many biotechnology companies. The increased interest in this class of targets reflects both advances in identifying selective protein kinase inhibitors and a growing perception that these drugs offer a novel, well-tolerated oral therapy in some of the most untreatable cancers.

Although direct kinase inhibitors accounted for only 7% of the value of the oncology market in 2006, their increasing availability and use is likely to be one of the major drivers of growth in this market.

The number of kinase inhibitors in clinical development ensures that during the next 10 years a significant number of such agents will reach the market. The majority of these will be for oncology indications, reflecting the more acute nature of the disease, and thus greater tolerability of potential side effects, and the current emphasis on developing kinase inhibitors for cancer indications.

About the author:
Peter Norman, PhD, MBA, is a pharmaceutical consultant and analyst based in Burnham Beeches, near Windsor, England. He has written and presented widely on various aspects of respiratory disease, drug development, and on the analysis of diverse therapeutic markets. Dr. Norman has more than 20 years of experience in the pharmaceutical industry in both R&D and competitive intelligence. His publications include many reviews and 16 original scientific papers and 11 patents, together with a number of industry reports, including the Insight Pharma Report, Metabolic and Inflammatory Disease R&D: An Assessment of 5 Highly Promising Therapeutic Classes, http://www.insightpharmareports.com/reports/2007/79_Metabolic/overview.asp. Dr. Norman holds science degrees from Cambridge University and Brunel University and an MBA degree from the Open University.