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MethylGene Presents Preclinical Data on MG516 at the American Association for Cancer Research Annual Meeting

Novel spectrum of targets for differentiated pipeline product

MONTREAL, CANADA--(Marketwired - April 8, 2013) - MethylGene Inc. (MYG.TO) today announced that preclinical data for the kinase inhibitor MG516 was presented at the American Association for Cancer Research (AACR) Annual Meeting held in Washington DC. In a poster entitled "Preclinical characterization of MG516, a novel inhibitor of receptor tyrosine kinases involved in resistance to targeted therapies" data was presented showing that MG516 possesses potent inhibitory activity against a spectrum of tyrosine kinase receptor targets including Eph receptors and Ret as well as Met, Axl and VEGF-R family members. The study incorporated data from in vitro kinase and cell-based analyses. In a broad variety of animal models of human cancer, MG516 demonstrated significant inhibition of tumor growth accompanied by suppression of the target kinases. MG516 also reversed resistance to the VEGFR inhibitor sunitinib in an in vivo preclinical tumor model.

"MG516 inhibits a novel spectrum of targets that have been shown to be drivers of tumor growth" said Dr. Charles Baum, President and Chief Executive Officer of MethylGene Inc. "This molecule is a valuable addition to MethylGene's oncology portfolio that is complementary to our MGCD265 program and has the potential to address unmet needs in patients with cancer".

About MG516

MG516 is a multi-targeted kinase inhibitor that covers a novel spectrum of targets including members of the Eph receptor family, the Met receptor, the Ret receptor tyrosine kinase, and all three vascular endothelial growth factor receptors (VEGFR 1, 2, 3). Eph is over-expressed in several cancers including gastric, breast, prostate and esophageal and is associated with resistance to HER2 inhibitors. Ret is expressed and has a role in medullary thyroid carcinoma, and recent data suggest a possible role as a driver of growth in lung cancer. MG516 has demonstrated potent inhibition of kinases in vitro, in multiple cell-based assays and has shown up to 100% of tumor growth inhibition in vivo against a number of tumor types in xenograft studies. In preclinical models anti-tumor activity is achieved at low doses and MG516 is well tolerated without significant weight loss or myelosuppression. MG516 is in advanced preclinical development and ready to commence IND-enabling studies.

About MethylGene

MethylGene Inc. (MYG.TO) is a drug development company that is advancing novel therapeutics for the treatment of patients with cancer and infectious disease in human clinical trials. The Company's lead clinical stage product candidates are: MGCD265, a multi-targeted receptor tyrosine kinase inhibitor that is in Phase I/II clinical trials for patients with solid tumors and MGCD290, an oral antifungal agent targeting the fungal Hos2 enzyme that was in Phase II trials for vulvovaginal candidiasis. MethylGene owns all rights to its lead product candidates, and has partnerships with Otsuka Pharmaceutical Co. Ltd., Taiho Pharmaceutical Co. Ltd., and EnVivo Pharmaceuticals, Inc. for its other pipeline programs.

Certain statements contained in this news release, other than statements of fact that are independently verifiable at the date hereof, may constitute forward-looking information and forward-looking statements (collectively "forward-looking statements" within the meaning of applicable securities laws). Such statements, based as they are on the current expectations of management of MethylGene and upon what management believes to be reasonable assumptions, inherently involve numerous risks and uncertainties, known and unknown, many of which are beyond MethylGene's control. Such statements can usually be identified by the use of words such as "may", "would", "believe", "plan", "estimate" and other similar terminology, or state that certain actions, events or results "may" or "would" be taken, occur or be achieved 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 our other programs; the ability to scale up, formulate and manufacture sufficient GMP, clinical or commercialization quantities of MGCD265, MGCD290 or our other products, 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 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, as described in MethylGene's Annual Information Form 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 news release. These statements speak only as of the date they are made and MethylGene expressly disclaims any duty, obligation or undertaking to release publicly any updates or revisions to any forward-looking statements contained herein to reflect any change in MethylGene's expectations with regard thereto of any change in events, conditions or circumstances on which any such statements are based except in accordance with law

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