MethylGene Presents MGCD290 Data at the 2012 Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC)

Montreal, Canada. September 11, 2012 – MethylGene Inc. (TSX:MYG) today announced that preclinical data for its novel clinical-stage antifungal, MGCD290, was presented at the 52nd 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.

Investor Relations Contact:

Joseph Walewicz, CFA

Vice President, Business & Corporate Development

MethylGene Inc.

Phone: 514-337-3333 ext. 373

ir@methylgene.com

www.methylgene.com

Thomas Hoffmann

Vice President

The Trout Group LLC

Phone: 646-378-2931

thoffmann@troutgroup.com

www.troutgroup.com

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