MethylGene presents results for HDAC inhibitors, multi-targeted kinase inhibitors

New York, April 4 - MethylGene Inc. reported positive data for in vivo studies to identify second generation HDAC inhibitors and multi-targeted kinase inhibitors.

In one announcement, the Montreal-based company presented preliminary results from a novel class of compounds designed to be used as second generation HDAC inhibitors in oncology.

The data demonstrated that these inhibitors increased potency and altered HDAC isoform selectivity profiles compared to first generation benzamide-based HDAC inhibitors, including MethylGene's MGCD0103 which is currently in human clinical trials.

Lead compounds were also shown to exhibit anti-tumor activity in in vivo models.

"In the near-term we will continue to evaluate these approaches in order to identify a second generation HDAC inhibitor clinical candidate in 2006," commented Jeffrey M. Besterman, MethylGene's executive vice president, research & development and chief scientific officer, in a news release.

The findings were presented in a poster at the 97th annual meeting of the American Association for Cancer Research in Washington, D.C.

In a second poster, MethylGene described its multi-targeted kinase inhibitors as having potent activity against the c-Met receptor and all three VEGF receptors, as well as having significant activity against RON, Tie-2 and Flt-3 kinases.

"Our ability to inhibit Flt-3 with our multi-targeted inhibitors is a recent achievement and provides another potential mechanism of action to these anticancer compounds." added Besterman.

The receptor c-Met and its ligand HGF are involved in tumor cell survival, tumor metastasis, and angiogenesis and have been shown to cooperate synergistically with VEGF receptors. RON, Tie-2 and Flt-3 are also known to play roles in either angiogenesis or tumor development.

The company's lead molecules were able to significantly suppress in vivo growth, and in some cases cause regression, of tumors in which c-Met is constitutively active, MethylGene reported.

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