MethylGene Inc.

MethylGene Inc.

April 04, 2006 14:14 ET

Methylgene Presents Second Generation HDAC and Multi-Targeted Kinase Preclinical Results at AACR Annual Meeting

MONTREAL, QUEBEC--(CCNMatthews - April 4, 2006) -

- In vivo and In vitro results presented in two poster sessions -

MethylGene Inc. (TSX:MYG) today disclosed preclinical data including in vivo efficacy results regarding the identification of second generation HDAC inhibitors and multi-targeted kinase inhibitors. The information was disclosed in two poster sessions which were displayed at the 97th American Association for Cancer Research (AACR) Annual Meeting in Washington, DC from April 1-5, 2006.

In a poster entitled "Enhanced Isotype-Selectivity and Antiproliferative Activity of Thiophenyl Derivatives of Benzamide HDAC Inhibitors In Human Cancer Cells," (abstract #4725), MethylGene presented preliminary results from a novel class of HDAC inhibitors. These compounds were 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, when 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.

"The data generated with our partners Pharmion Corporation and Taiho Pharmaceutical suggest that we have new chemical approaches to the discovery of second generation HDAC inhibitors and that we can cover additional chemical space with these patent-pending approaches." commented Dr. Jeffrey M. Besterman, MethylGene's Executive Vice President, Research & Development and Chief Scientific Officer. "In the near-term we will continue to evaluate these approaches in order to identify a second generation HDAC inhibitor clinical candidate in 2006."

In a second poster entitled "Evaluation of antitumor activity, anti-angiogenic activity and pharmacodynamic end-points for orally active multi-targeted anti-angiogenic kinase inhibitors targeting c-MET, RON, VEGF and Tie-2 receptors," (abstract #246) the Company 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 Dr. 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. Most notably, 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. These compounds appear to have broad spectrum anti-tumor activity with no significant body weight loss or bone marrow suppressive effects. Furthermore, in vivo models were evaluated for several pharmacodynamic end-points including the auto-phosphorylation of c-met, Tie-2, VEGFR2 and ERK, (a downstream marker of signal transduction regulation). The data demonstrated that a reduction in auto-phosphorylation activity of these targets correlated with the inhibition of angiogenesis and anti-tumor activity. The Company expects to continue advancing this program with the goal to identify a clinical candidate in 2006.

About MethylGene

MethylGene is a publicly-traded biopharmaceutical company focused on the discovery, development and commercialization of novel therapeutics in cancer and infectious diseases. We intend to exploit our HDAC inhibitor technology in other diseases, such as diabetes, inflammation, fungal infections and neurodegenerative disorders. Two cancer product candidates are currently in clinical trials: MGCD0103, partnered with Pharmion Corporation and Taiho Pharmaceutical Co., Ltd., and MG98, partnered with MGI Pharma, Inc. MethylGene has an exclusive license agreement with Merck & Co. for the development and commercialization of small molecule beta-lactamase inhibitors to overcome antibiotic resistance. MethylGene has partnered its non-oncology HDAC program for neurodegenerative diseases with EnVivo Pharmaceuticals. MethylGene has a portfolio of preclinical programs for its multi-targeted kinase and histone deacetylase (HDAC) inhibitors for both oncology and non-oncology indications, and continues to seek partnering opportunities in these areas. Please visit our website at

Certain statements contained in this news release, other than statements of fact that are independently verifiable at the date hereof, may constitute forward-looking statements. Such statements, based as they are on the current expectations of management of MethylGene, inherently involve numerous risks and uncertainties, known and unknown, many of which are beyond MethylGene's control. Such risks include, but are not limited to, the impact of general economic conditions, economic conditions in the pharmaceutical industry, changes in the regulatory environment in the jurisdictions in which MethylGene does business, stock market volatility, fluctuations in costs, expectations with respect to our intellectual property position and our ability to protect our intellectual property and operate our business without infringing upon the intellectual property rights of others, changes in the competitive landscape including changes in the standard of care for the various indications in which MethylGene is involved, and changes to the competitive environment due to consolidation, as well as other risks, which you are urged to read, as described in MethylGene's Annual Information Form for the fiscal year ending December 31 2005, under the heading "risk factors," that can be found at Consequently, actual future results may differ materially from the anticipated results expressed in the forward-looking statements. The reader should not place undue reliance on the forward-looking statements included in this presentation. These statements speak only as an update on the date they are made and MethylGene is under no obligation to revise such statements as a result of any event, circumstance or otherwise except in accordance with law.

Contact Information

  • MethylGene Inc.
    Andrea Gilpin, Ph.D, MBA
    Director, Investor Relations & Project Management
    (514) 337-3333 ext.416