MethylGene Reports Progress on Isotypic Selective HDAC Inhibitor Chemistries for Oncology.

Business Editors/Health/Medical Writers

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MONTREAL--(BUSINESS WIRE)--Oct. 27, 2003

MethylGene Inc., a private Canadian drug discovery and development company focused in cancer and infectious diseases, publishes two chemistry papers on histone deacetylase (HDAC) inhibitors for oncology.

The field of HDAC inhibitors has emerged as a novel human anticancer strategy and MethylGene has developed multiple classes of small molecule inhibitors against HDACs. In two chemistry papers in Current Medicinal Chemistry (Curr. Med. Chem., 2003, Vol. 10, 2359-2372) and Bioorganic Medicinal Chemistry Letters (in press and scheduled to appear in Vol. 14 Issue 1), the Company describes its recent progress in the development of HDAC inhibitors for oncology, which includes hydroxamic acids, anilides, TSA-like straight chain derivatives, and 2-aminophenylamides of omega-substituted alkanoic acids. These inhibitors preferentially inhibit cancer cell proliferation, cause cancer cell cycle arrest, and induce apoptosis.

HDACs are a family of enzymes that regulate gene expression. In cancer, they are overexpressed and specifically turn off tumor suppressor genes. "Such scientific publications are another milestone in our effort to position MethylGene as a leader in the design of isotypic enzyme inhibitors," said Dr. Jeffrey Besterman, Senior Vice President, Research and Development.

Recently, MethylGene announced a collaboration and license agreement with Taiho Pharmaceutical Co., Ltd., a leading Japanese oncology specialty company, on its small molecule inhibitor HDAC program for oncology. In the deal worth US$37.5 million, MethylGene received an upfront of US$3.75 million and research and development funding support in North America. Taiho is responsible for development of an HDAC oncology product in Japan, Korea, Taiwan, and China and MethylGene will receive royalties based on sales of an HDAC oncology product in these countries.

MethylGene's clinical candidate MGCD0103 is an HDAC inhibitor for oncology and is currently in GLP toxicity studies. An IND is expected to be filed at the end of this year. This compound exhibits significant antitumor activity in a variety of in vivo tumor models including prostate, lung, colon, pancreatic, and ovarian cancers. In addition, it has a good toxicity profile and therapeutic window, is orally available, and is selective for HDAC isotypes involved in cancer.

About MethylGene

MethylGene Inc. is a privately-held Canadian biopharmaceutical company engaged in the discovery and development of novel and proprietary drugs to treat cancer and infectious diseases. MG98, MethylGene's lead anti-cancer compound, is currently in clinical trials and is partnered with MGI PHARMA, Inc. in North America and with British Biotech plc/Vernalis in Europe. The Company's second oncology product, MGCD0103, is an orally active, isoform selective, small molecule inhibitor of histone deacetylase for oncology for which an IND is expected to be filed later this year. A small molecule beta-lactamase program to overcome antibiotic resistance was recently partnered with Merck Frosst & Co. for worldwide rights. In addition, the Company has a portfolio of other chemistry driven research programs including HDAC inhibitors for other non-oncology focused large market indications. For more information about MethylGene, please visit www.methylgene.com.

This press release may contain forward-looking statements pertaining to MethylGene Inc. Such statements are subject to certain risk factors and uncertainties, particularly those inherent in the process of discovering, researching, developing and commercializing drugs that can be proven to be safe and effective for use as human therapeutics and the endeavor of building a business around such potential products. As a result, the reader is cautioned that actual results could differ materially from those projected or assumed around this release.