Abstract
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.