MONTREAL, QUEBEC, CANADA--(Marketwire - Sept. 11, 2012) - MethylGene Inc. (TSX:MYG) today announced that preclinical data for its novel clinical-stage antifungal, MGCD290, was presented at the 52^nd Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) taking place in San Francisco, California. The poster, entitled "MGCD290, an Oral Fungal Hos2 Inhibitor, Enhances the Antifungal Properties of Fluconazole following Multiple or Single Oral Dose Administration in Pre- and Post-Infection Settings" (Presentation #M-1711), demonstrated that MGCD290 plus fluconazole was superior to fluconazole alone in a murine model of systemic candidiasis under multiple dosing schedules.

Fluconazole is the most widely used triazole antifungal, and previous in vitro and in vivo studies have established that MGCD290 enhances the antifungal activity of fluconazole, broadening its spectrum of activity and increasing the sensitivity of fungi to fluconazole.

Today's poster details how, under different dosing schedules in a mouse model of systemic candidiasis, the combination of MGCD290 plus fluconazole significantly decreased the fungal kidney burden versus fluconazole alone. The combination of MGCD290 plus fluconazole was superior in both fluconazole-sensitive candidiasis and fluconazole-resistant candidiasis. Dosing schedules tested included a single dose of fluconazole plus MGCD290 administered after infection, or prophylactic dosing followed by a second post-infection treatment.

"The preclinical data reported today demonstrates the activity of MGCD290 under conditions relevant to mucosal and life-threatening systemic antifungal indications, as well as supporting the ability of MGCD290 to overcome azole resistance, an increasing problem." said Dr. Jeffrey Besterman, MethylGene's Executive Vice President, Research and Development and Chief Scientific Officer.

Enrollment in MethylGene's randomized, multicenter, blinded, placebo-controlled, Phase II trial in the U.S. is over 50% complete. This study is evaluating MGCD290 plus fluconazole versus fluconazole alone in patients with moderate to severe vulvovaginal candidiasis (VVC), a form of yeast infection for which current treatments have limited efficacy. Topline data from this trial is expected around the end of 2012.

MGCD290 Investor Event

MethylGene will host an investor event focused on trends in fungal disease and the novel antifungal therapeutic, MGCD290, on Wednesday, October 10th, 2012 at 8.00-10.00 a.m. in New York, New York. The event will also be available by live webcast.

About MGCD290

MGCD290 is a first-in-class, orally available, small molecule inhibitor of the fungal enzyme Hos2. Current antifungal therapies suffer from a number of shortcomings including gaps in the coverage of fungal pathogens, acquisition of resistance, toxicity and drug-drug interactions. MGCD290 is initially being developed as a combination product with fluconazole, the most widely used triazole antifungal. In vitro, MGCD290 in combination with fluconazole reverses fluconazole resistance (primary and acquired) in a wide range of fungal species, including Candida glabrata. MGCD290 has completed multiple Phase I studies in healthy adult volunteers and has shown an excellent safety profile without drug-drug interactions, either as monotherapy or in combination with fluconazole. A randomized, controlled Phase II study in moderate to severe VVC is underway.

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 presentation. These statements speak only as an update on 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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