MethylGene and Otsuka Pharmaceutical Co., Ltd. Extend Funded Research Collaboration; Methylgene Could get up to $50.5 Million

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MONTREAL, QUEBEC--(Marketwire - 09/09/09) - MethylGene Inc. announced that Otsuka Pharmaceutical Co. Ltd. has extended its funded research collaboration with MethylGene for the development of novel, small molecule, kinase inhibitors for the local delivery and treatment of ocular diseases, excluding cancer, for an additional six months. As part of the collaboration that was initially formed in March 2008, MethylGene received a US$2 million upfront license fee and may be eligible to receive additional payments based on the successful development, regulatory, commercialization and sales milestones that could total US$50.5 million. MethylGene will also receive royalties on net sales of any resulting product.

With the extension, Otsuka will provide an additional US$625,000 to MethylGene in research funding for the six-month period ending March 2010. Otsuka also maintains its right to further extend the collaboration beyond this incremental six-month period. In addition, Otsuka will make a US$1.5 million equity investment in MethylGene, per the terms of the original agreement, by the end of October.

MethylGene will continue to design, synthesize, characterize and screen kinase inhibitors and Otsuka will fund efficacy and toxicology studies, as well as the preclinical and clinical development of compounds. To date, the collaboration efforts have led to the identification of lead compounds for ocular diseases that have demonstrated efficacy and safety in various in vivo models. The extended collaboration will focus on the identification of optimized leads and additional leads with potentially enhanced properties. Otsuka will provide additional assistance in the scale-up of selected compounds and preclinical development in multiple in vivo settings for both efficacy and safety. Otsuka remains solely responsible for the clinical development and global commercialization of any resulting product.

“We are pleased Otsuka has extended our productive collaborative research effort,” said Donald F. Corcoran, President and Chief Executive Officer of MethylGene Inc. “Our ability to develop kinase inhibitors for use in treatments beyond cancer demonstrates MethylGene’s strength in this growing field of research. We look forward to continuing to provide Otsuka with potent kinase inhibitors with the goal of identifying a clinical candidate.”

About MethylGene

MethylGene Inc. (TSX:MYG - News) is a publicly-traded, clinical stage, biopharmaceutical company focused on the discovery, development and commercialization of novel therapeutics with a focus on cancer. The Company’s product candidates include: MGCD265, an oral, multi-targeted kinase inhibitor targeting the c-Met, VEGF, Ron and Tie-2 receptor tyrosine kinases that is in Phase II clinical trials for cancers; MGCD290, a fungal Hos2 (HDAC) inhibitor being developed for use in combination with fluconazole for serious fungal infections that is 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.

Contacts: Investor Relations Contacts: Rx Communications Group, LLC Rhonda Chiger 917-322-2569 rchiger@rxir.com MethylGene Inc. Donald F. Corcoran President & CEO 514-337-3333 ext. 373 mctavishk@methylgene.com www.methylgene.com

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