MONTREAL, CANADA--(Marketwire - Oct. 22, 2012) - MethylGene Inc. (TSX:MYG) today announced that Phase I data for its novel clinical-stage antifungal, MGCD290, were presented at the 2012 IDWeek™ meeting, held in San Diego, California from October 17-21, 2012. Data describing the safety and pharmacokinetics of MGCD290 in four Phase I clinical trials in healthy adult volunteers were presented in a poster entitled "Safety and Pharmacokinetics of MGCD290, an Oral fungal Hos2 Inhibitor, Alone and in Combination with Fluconazole: Single and Multiple Ascending Dose Studies in Healthy Subjects (290-001, 002, 003, 004)" (presentation #1619).

Previous preclinical studies have established that MGCD290 enhances the antifungal activity of fluconazole, broadening its spectrum of activity and increasing the sensitivity of fungi to fluconazole. Data presented at the 2012 IDWeek™ described the safety profile of MGCD290 in humans under different dosing schedules and in the presence or absence of fluconazole. MGCD290 monotherapy was tested up to 1000 mg as a single dose and up to 540 mg daily in 14 day repeat dose studies (studies 290-001, 290-002). MGCD290 in combination with 400 mg fluconazole was tested up to 540 mg daily for 14 days (studies 290-003, 290-004). All doses and schedules tested were well tolerated, with no severe or serious adverse events reported. Pharmacokinetics were dose-dependent and MGCD290 demonstrated a large apparent volume of distribution and good tissue penetration. No drug-drug interactions were observed between MGCD290 and fluconazole.

"Data from these Phase I studies indicate that MGCD290 has an attractive pharmacokinetic and safety profile, supporting its ongoing clinical development," said Dr. Rachel Humphrey, Executive Vice President and Chief Medical Officer of MethylGene. "We continue to be encouraged by the potential of this drug for vulvovaginal candidiasis and other indications such as systemic or invasive fungal infections."

A randomized, placebo-controlled, double-blind, multi-center, Phase II trial is underway to evaluate MGCD290 plus fluconazole versus fluconazole alone in patients with moderate to severe vulvovaginal candidiasis (VVC). Topline data from this trial is expected in Q1 2013.

About MGCD290

MGCD290 is a first-in-class, orally available, small molecule inhibitor of the fungal enzyme Hos2. In preclinical models the combination with azole antifungal agents results in broader coverage of fungal pathogens and decreases resistance to the most widely used antifungal agents. MGCD290 is 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 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 drug development company that is advancing 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 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 patients with solid tumors. 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.

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