Methylgene Receives Clinical Trial Approval from Health Canada for its Proprietary Product Candidate MGCD290 for Fungal Infections

- Phase I clinical study planned to begin in October 2008 - MGCD290 enhances the spectrum of antifungal azole activity including azole-resistant fungal strains

MethylGene Inc. (TSX: MYG) today announced that Health Canada has approved the Company's clinical trial application (CTA) for MGCD290, a fungal Hos2 histone deacetylase (HDAC) inhibitor to be used in combination with azoles for the treatment of fungal infections.

MethylGene expects to initiate a Phase I clinical trial in Canada in October of this year. The goal of this trial will be to assess the safety, pharmacokinetics and tolerability of the compound in healthy volunteers. MGCD290 will initially be administered orally as a single-agent and, in future planned studies, in combination with oral fluconazole, a widely used antifungal agent. In preclinical studies, MGCD290 in combination with fluconazole increased fungal sensitivity and broadened the spectrum of azole activity in vitro against human fungal pathogens, including azole-resistant clinical isolates.

"We are pleased to have received approval to commence this study for MGCD290, which will be our third small molecule in clinical development," said Donald F. Corcoran, President and Chief Executive Officer of MethylGene. "MGCD290 is our first HDAC inhibitor for use outside of oncology. MGCD290 differs from our anticancer HDAC compounds in that it targets the fungal enzyme, Hos2, that is distinct from human HDACs. In addition, it is from a different chemical family than that of our current cancer compounds."

MGCD290 is designed to be co-administered with azoles, in particular fluconazole, to potentiate and enhance azole activity against fungal infections. The need to develop novel, broad-spectrum antifungal agents is particularly important due to emerging resistance and the desire to broaden the spectrum of a number of currently utilized azoles.

Joint 48th Annual ICAAC / IDSA 46th Annual Meeting

MethylGene will disclose additional preclinical data for MGCD290 in two poster presentations at the joint 48th Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) / Infectious Disease Society of America (IDSA) 46th Annual Meeting to be held in Washington, DC from October 25 to 28, 2008. The posters will be presented on October 27 from 10:00 a.m. to 4:30 p.m. ET.

Title: In vivo properties of MGCD290, an antifungal Hos2 histone deacetylase (HDAC) enzyme inhibitor.

Presentation Number: M-2133

Title: Combination testing of MGCD290, a fungal histone deacetylase inhibitor, with azole antifungals against a large collection of clinical fungal isolates.

Presentation Number: M-2129

About MGCD290

MGCD290 is an oral, small molecule, fungal Hos2 histone deacetylase (HDAC) inhibitor that appears to target fungal HDACs preferentially to human HDACs. MGCD290 potentiates and broadens the spectrum of azole activity against human fungal pathogens, including azole-resistant isolates. Treatment with azoles, a commonly used class of drugs for fungal infections, often results in the emergence of resistant fungal strains, thereby rendering the azole treatment ineffective over time. It is believed that the fungi may become resistant to azole treatment through the action of certain fungal HDAC isoforms, which affect the expression of key fungal genes conferring resistance to azoles. The demand for effective antifungals is driven by a rising incidence of immunocompromised patients including individuals with cancer who are receiving chemotherapy treatment and/or transplants.

About MethylGene

MethylGene Inc. (TSX: MYG) is a publicly-traded, clinical stage, biopharmaceutical company focused on the discovery, development and commercialization of novel therapeutics for cancer. The Company's product candidates include: MGCD265, an oral, multi-targeted kinase inhibitor targeting the c-Met, Tie-2, Ron and VEGF receptor tyrosine kinases and is in Phase I clinical trials for solid tumor cancers; MGCD290, a fungal Hos2 (HDAC) inhibitor used in combination with azoles for fungal infections; and MGCD0103, an oral, isoform-selective HDAC inhibitor which has been in multiple clinical trials for solid tumors and hematological malignancies and is licensed to Celgene Corporation and Taiho Pharmaceutical. In addition, MethylGene's preclinical programs include: a kinase inhibitor program for ocular diseases and a sirtuin inhibitor program for cancer. MethylGene's development and commercialization partners include Celgene Corporation, Taiho Pharmaceutical Co. Ltd., Otsuka Pharmaceutical Co. Ltd. and EnVivo Pharmaceuticals. Please visit our website at www.methylgene.com.

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. These risks and uncertainties could cause future results, performance or achievements to differ significantly from the results, performance or achievements expressed or implied by such forward-looking statements. Such results, performance or achievements include, but are not limited to, the timing and effects of regulatory action; the continuation of collaborations; the results of clinical trials; the timing of enrollment or completion of clinical trials; the success, efficacy or safety of MGCD0103, MGCD265 or MGCD290; the ability to scale up, formulate and manufacture sufficient GMP, clinical or commercialization quantities of MGCD0103, MGCD265 or MGCD290, and the relative success or the lack of success in developing and gaining regulatory approval and/or market acceptance for any compound or new product including MGCD0103, MGCD265 or MGCD290. 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, 2007, under the heading 'risk factors,', and all other documents filed by the Company that can be found at www.sedar.com. 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.

Contacts: Investor Relations Contacts: Rx Communications Group, LLC Rhonda Chiger 917-322-2569 This email address is being protected from spambots. You need JavaScript enabled to view it. MethylGene Inc. Donald F. Corcoran President & CEO 514-337-3333 ext. 373 This email address is being protected from spambots. You need JavaScript enabled to view it.

SOURCE: MethylGene Inc.

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