MethylGene Announces Change of President and CEO

MONTREAL, QUEBEC--(Marketwire - Sep 24, 2012) - MethylGene Inc. ("MethylGene" or the "Company") (TSX:MYG) announced today that Mr. Charles Grubsztajn has left the Company as President and Chief Executive Officer effective immediately and will resign as director of the Company. Dr. Martin Godbout, Chairman of the Board of MethylGene, will assume the role of President and Chief Executive Officer on an interim basis as the Company concludes its executive search process. An announcement to that effect is expected shortly.

Dr. Godbout stated: "On behalf of MethylGene, I would like to thank Charles for his leadership of the Company through a challenging period. He attracted the capital and the talent to successfully position MethylGene for aggressive growth and value creation. We wish him every success in his future endeavours."

About MethylGene

MethylGene Inc. (TSX:MYG) is a small molecule drug development company that is advancing two novel therapeutics for cancer and infectious disease in human clinical trials. The Company''s lead product candidates are: MGCD290, an oral antifungal agent targeting the fungal Hos2 enzyme that is currently in Phase II trials for vulvovaginal candidiasis, and MGCD265, an oral Met/VEGF receptor kinase inhibitor that is in Phase I/II clinical trials for solid tumor cancers. 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 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 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.

Contact:

MethylGene Inc.

Joseph Walewicz, CFA

Vice President, Business & Corporate Development

514-337-3333 ext. 373

ir@methylgene.com

www.methylgene.com

The Trout Group LLC

Thomas Hoffmann

Vice President

646-378-2931

thoffmann@troutgroup.com

www.troutgroup.com

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