Report predicts kinase market to reach $58.6bn in 2010

The report explores a lucrative market in which the last five years have seen eight anticancer kinase inhibitors receiving FDA approval, increasing recognition of kinases as a vital drug target class.

The report, compiled by Pharmaprojects, involved carrying out numerous surveys, which included a search of Pharmaprojects, a database tracking pharmaceutical R&D worldwide.

In addition, a survey of the last six years of kinase-related patenting at the US PTO was conducted as well as an on-line survey of pharmaceutical industry and academic personnel.

The results left observers in no doubt of the strength of this market, buoyed on by the prospect of more innovative biotherapeutic-targeting kinases that can be expected over the next 10-15 years.

The Pharmaprojects database search generated 803 drug profiles representing 243 unique companies, 184 unique targets, and 68 unique indications/drug types.

A subsequent search of the Entrez Gene database for human genes with kinase activity led the researchers to conclude that 145 kinase-related genes are currently drug targets, while 627 kinase-related genes remain unexplored as drug targets.

Additional examination of the Pharmaprojects dataset revealed that the kinase drug market is at a relatively early stage. The study also revealed that overall 80 per cent of drugs are still in preclinical development.

By far the largest indication for kinase-targeted drugs, almost 41 per cent of the total, is cancer.

Of the top five kinase drug targets, only one is not primarily a cancer target. Other important indications for kinase-targeted drugs include inflammation, arthritis, diabetes, and cardiovascular disease.

Of the top ten companies most active in this area, only Pfizer, Novartis, AstraZeneca, and GlaxoSmithKline have launched products.

Currently, the emphasis is on small molecule approaches to kinase inhibition. The majority of the respondents to our on-line survey felt that small molecule inhibitors were preferable to monoclonal antibodies and that multi-target kinase inhibitors were more likely to prove commercially successful than single-target inhibitors.

Now that many kinases have been sequenced and their structures have been determined, more efficient approaches to small molecule kinase inhibitor discovery are urgently needed.

Kinases with a particular focus on the development of new assays for use in high throughput screening for potential inhibitors, specificity profiling of candidate drugs, and identifying physiological substrates of targeted kinases.

Despite the current focus on small molecule inhibitors, the industry appears to be moving toward a more balanced portfolio of small molecules and biopharmaceuticals.

According to Pharmaprojects, more than 20 per cent of kinase-targeted drugs in development, especially those addressing cancer are biopharmaceuticals.

Our patent search identified 3,687 kinase-related US patents and patent applications filed since January 2000 and revealed that they are being filed at a steady rate of around 730 per year.

The report fund that a large proportion of late-stage clinical trials targeted receptor tyrosine kinases.

The discovery of activating and resistance mutations has fuelled the drive towards mutation-specific therapies that could provide patients with a drug that matches the genetic profile of their biopsied tumour.

While some companies endeavour to design highly selective single target inhibitors, others are developing multi-target kinase inhibitors. Companies taking the latter approach can screen drugs for desirable effects on cancer processes such as proliferation or angiogenesis which are mediated by kinases frequently mutated or over expressed in tumours, without investing heavily in the technologies needed to develop highly selective drugs.

Outside of cancer, the only launched drugs are agents, which were not developed with kinase modulation in mind, but are now known to affect disease-associated kinases.

The report concluded that although kinase targeted drugs are currently under investigation for over 50 unique indications, most commercial activity centred on the areas of inflammation and tissue injury, diabetes and cardiovascular disease.

The report: "Kinases: Advanced Strategies and Multiple Targets for Drug Discovery," is available now from D&MD Publications.