MethylGene Presents Preclinical Data for Its Second Oral Kinase Inhibitor, MG516, at the American Association for Cancer Research Annual Meeting

MONTREAL, QUEBEC--(Marketwire - April 21, 2009) - MethylGene Inc. (TSX: MYG) today disclosed preclinical data for its potential clinical candidate, MG516, a second generation multi-targeted kinase inhibitor from the Company’s proprietary oncology kinase program. MG516 inhibits a novel spectrum of targets which include members of the Eph receptor family, the Ret receptor tyrosine kinase, c-Met and all three vascular endothelial growth factor receptors (VEGFR 1, 2 3). The inclusion of Eph and Ret as targets is important due to their overexpression and/or mutation in a number of cancers. Eph is overexpressed in several cancers including gastric, lung, breast, ovarian, brain and skin while the activating mutations of Ret are primarily associated with medullary thyroid carcinoma (MTC). The data for MG516 were presented in a poster session at the American Association for Cancer Research (AACR) Annual Meeting in Colorado.

In a poster entitled “Preclinical Development of a Novel Oral Multi-targeted Kinase Inhibitor with Potent in vivo Anti-tumor Activity,” (poster #3731) results from in vivo human tumor models in mice demonstrated dramatic inhibition of tumor growth in a broad range of cancer types at very low, once per day, oral doses. MG516 demonstrated tumor regression in a number of cases and inhibited tumor growth by 80 to 100 percent in colorectal carcinoma, leiomyosarcoma, medullary thyroid, gastric carcinomas and glioblastoma tumor models. These potent anti-tumor activities were achieved at oral doses as low as 5mg/kg and in the absence of overt toxicity, weight loss or myelosuppressive events. MG516 showed pharmacodynamic inhibition of target phosphorylation in vivo in human tumor models and demonstrated dose-dependent inhibition of the plasma markers VEGF and HGF. In summary, it appears that MG516 targets a novel spectrum of enzymes, has an impressive anti-tumor profile, a wide therapeutic window and a potential for clinical development in a variety of cancer types.

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, VEGF, Tie-2 and Ron receptor tyrosine kinases that is in Phase I clinical trials for solid tumor cancers; MGCD290, a fungal Hos2 (HDAC) inhibitor being developed for use in combination with fluconazole for serious fungal infections that is also in Phase I clinical studies; 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 Taiho Pharmaceutical Co. Ltd. A fourth compound discovered using MethylGene’s HDAC platform, EVP-0334 - a potential cognition enhancing agent, is in a Phase I study sponsored by EnVivo Pharmaceuticals Inc. MethylGene also has a funded collaboration with Otsuka Pharmaceutical Co. Ltd. for applications in ocular diseases using the Company’s proprietary kinase inhibitor chemistry. 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, 2008, 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.