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MONTREAL, QUEBEC--(Marketwire - April 5, 2011) -MethylGene Inc.(TSX:MYG) today disclosed preclinical data during a presentation for its proprietary Met/VEGFR kinase inhibitor, MGCD265, at the AACR 102^nd Annual meeting held in Orlando, Florida.

MGCD265 is currently being investigated in multiple clinical trials including a combination trial with docetaxel (Taxotere®). MGCD265 primarily targets Met and VEGFR and blocks activities which contribute to cancer development and progression such as cell proliferation, motility, angiogenesis and tumor cell survival.

In a poster presentation entitled "Potent Preclinical Anti-tumor Activity of MGCD265, an Oral Met/VEGFR Multi-targeted Receptor Tyrosine Kinase Inhibitor in Clinical Development, in Combination with Taxanes," (poster no. 27) results demonstrate that the combination of MGCD265 with docetaxel or with paclitaxel achieved greater anti-tumor responses compared to the antitumor activity of either agent alone. The combination of MGCD265 with either taxane was well tolerated and did not result in drug-drug interactions. Studies presented were aimed at gaining insight into the molecular basis for the synergistic activity of MGCD265 with docetaxel. In addition to altering tumor vasculature, combining MGCD265 with docetaxel resulted in improved inhibition of tumor proliferation. Gene expression profiles from human tumor xenografts treated with MGCD265 and docetaxel further revealed that genes regulated by either agent alone could be simultaneously regulated in the combination and that genes not altered by either agent alone could be modulated when the two agents were combined, including genes involved in anti-tumor functions.

The results presented not only demonstrate the anti-tumor activities of MGCD265 but provide a rationale for combining MGCD265 with taxanes. This rationale is further supported by the often high expression and phosphorylation/activation of Met in cancer, including in non-small cell lung cancer, and the common utilization of taxanes as chemotherapeutic agents. As reported recently, ongoing clinical trials indicate that MGCD265 can be combined safely with full dose docetaxel and this combination showed early signs of efficacy. An update on clinical activities of MGCD265 is anticipated at an upcoming medical meeting.

About MGCD265

MGCD265 is a novel, orally active small molecule inhibitor that targets a unique spectrum of receptor tyrosine kinases: Met, VEGFR 1, 2, and 3, Tie-2 and Ron. These kinases play key roles in tumor development, survival and metastasis as well as the inappropriate formation of blood vessels (angiogenesis) that nourish the tumor. MGCD265 is nearing completion of two Phase 1 single agent clinical trials and one Phase 1/2 combination clinical trial (with erlotinib and docetaxel) in solid tumors.

About MethylGene

MethylGene Inc. (TSX:MYG) is a clinical-stage biopharmaceutical company that develops novel therapeutics for cancer and infectious disease. The Company's lead product candidates include: MGCD265, an oral Met/VEGFR kinase inhibitor that is in Phase 1/2 clinical trials for solid tumor cancers and MGCD290, a fungal Hos2 inhibitor, for use in combination with fluconazole for fungal infections, which has completed Phase 1 clinical studies. The Company's partners include Otsuka Pharmaceutical Co. Ltd., Taiho Pharmaceutical Co. Ltd., and EnVivo Pharmaceuticals, Inc.

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 MGCD265, MGCD290 or mocetinostat (MGCD0103); the ability to scale up, formulate and manufacture sufficient GMP, clinical or commercialization quantities of MGCD265, MGCD290 or mocetinostat, 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 MGCD265, MGCD290 or mocetinostat. 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, as described in MethylGene's Annual Information Form for the fiscal year ending December 31, 2010, under the heading "Risk Factors" which you are urged to read 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.