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Published on 11/16/2005 in the Prospect News Biotech Daily.

MethylGene's kinase inhibitors disrupt tumor growth and blood vessel formation, preclinical data shows

By Angela McDaniels

Seattle, Nov. 16 - MethylGene Inc. said preclinical results show that its multi-targeted kinase inhibitors exhibit antitumor efficacy and disrupt tumor blood vessel formation.

Other findings include:

• The inhibitors can be taken orally, have low nanomolar potency against target enzymes, show no overt toxicity and have broad-spectrum antitumor activity in vivo at well-tolerated doses.

• The inhibitors target c-met receptor targets, all three VEGF receptor targets, Tie-2 kinases and Ron kinases, all of which are involved in tumor development.

• The inhibitors consistently demonstrate equal or superior oral antitumor efficacy compared to several competitor tumor blood vessel formation inhibitors which are currently in late-stage clinical trials.

• Some of the inhibitors have properties that allow for testing in ophthalmologic applications.

The data was presented during the European Organization for Research and Treatment of Cancer, National Cancer Institute and American Association for Cancer Research International Conference on Molecular Targets and Cancer Therapeutics in Philadelphia.

Proof-of-concept testing has begun with an undisclosed eye care company, the company said. MethylGene's goal is to have identified a clinical candidate for an Investigational New Drug Application and to begin studies in three to nine months.

Given the market success of anticancer kinase inhibitors such as Gleevec, Erbitux, Avastin and Herceptin, the company said there is an intense interest in targeting kinases.

MethylGene is a Montreal-based biopharmaceutical company that develops therapeutics for cancer and infectious diseases.


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