MethylGene Presents Phase I Data for Its Novel Antifungal Agent, MGCD290, at the 50th Annual ICAAC Meeting

MONTREAL, QUEBEC--(Marketwire - September 13, 2010) - MethylGene Inc. (TSX: MYG) today reported final data from its completed MGCD290 Phase I clinical trials. MGCD290 is an oral, small molecule, Hos2 fungal inhibitor for use in combination with azoles, such as fluconazole, for fungal infections. The data were presented in a poster session at the 50th Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) in Boston, Massachusetts.

Poster F1-862: Multiple Ascending Dose Phase I Studies in Healthy Subjects Demonstrate Safety and Pharmacokinetics of MGCD290, an Oral Fungal Hos2 Inhibitor +/- Fluconazole

Favorable data demonstrating the safety of the compound, as well as favorable pharmacokinetic properties were reported from two repeat-dose MGCD290 clinical studies (Trials 290-003 and 290-004). The randomized, double-blind, placebo-controlled studies were performed in a total of 48 healthy adult volunteers. Subjects enrolled were administered MGCD290 or a placebo. The trial design was eight subjects per cohort - six were administered MGCD290 and two were given the placebo.

The objectives of the Phase I studies were to determine the tolerability and pharmacokinetics of MGCD290 when administered daily for 14 days as a single agent (Trial 290-003) or in combination with fluconazole (Trial 290-004).

In Trial 290-003, 32 subjects were enrolled. Subjects received oral doses of MGCD290 as a single agent ranging from 100mg to 540mg daily for 14 days. There were no clinically significant drug-related adverse events observed at any of the dose levels and no-dose limiting toxicities were identified. The maximal plasma concentrations were observed approximately two hours after oral drug intake with a mean elimination half life of approximately nine hours.

Sixteen subjects were enrolled in Trial 290-004 and received MGCD290 or placebo in combination with fluconazole. Subjects were given daily, oral doses of 270mg or 540mg of MGCD290, along with a fixed dose of 400mg of fluconazole for 14 days. Data from this trial demonstrated that MGCD290 in combination with fluconazole was well-tolerated without any evidence of drug-drug interactions. There were no clinically significant drug-related adverse events observed at any of the dose levels and no-dose limiting toxicities were identified. In addition, pharmacokinetic data suggests that clinically relevant plasma concentrations of MGCD290 are achievable and safe when given in combination with 400mg of fluconazole.

All MGCD290 Phase I first in human clinical studies are now complete. Studies have demonstrated the safety of the agent and the favorable pharmacokinetic properties when administered alone or in combination with fluconazole. In addition, no serious adverse events were reported.

About MGCD290

MGCD290 is the lead compound from a proprietary class of small molecules that potentiates and extends the antifungal spectrum of azoles, and restores susceptibility to azole-resistant fungal pathogens. The addition of MGCD290 to fluconazole, the most widely prescribed azole, has been shown to intensify the cidality and increase the potency of fluconazole by up to 1000-fold in yeasts, molds, and dermatophytes. In addition, MGCD290 expands fluconazole’s spectrum of activity and restores susceptibility to pathogens such as C. glabrata, C. krusei, and Zygomycetes which are clinically resistant to fluconazole, and cross-resistant to azoles. In preclinical and clinical studies to date, MGCD290 in combination with fluconazole has shown an excellent safety profile, linear pharmacokinetics, and no drug-drug interactions. The Company believes that MGCD290 may be combined with any azole, and has the potential to be administered orally, IV, and topically. As such, the compound may have broad commercial appeal for treatment of invasive fungal infections and onychomycosis.

About MethylGene

MethylGene Inc. (TSX: MYG) is a publicly-traded, clinical stage biopharmaceutical company focused on the 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 Met, VEGF, Ron and Tie-2 receptor tyrosine kinases that is in multiple clinical trials for cancer; MGCD290, a fungal Hos2 inhibitor for use in combination with fluconazole for serious fungal infections which has completed Phase I clinical studies; and mocetinostat (MGCD0103), an oral, isoform-selective HDAC inhibitor for cancer which has been in multiple Phase II clinical trials and is currently in a Phase II trial in refractory or relapsed follicular lymphoma. Mocetinostat is licensed to Taiho Pharmaceutical Co. Ltd in certain Asian countries. A fourth compound discovered using MethylGene’s HDAC platform, EVP-0334 - a potential cognition enhancing agent for neurodegenerative diseases has successfully completed Phase I trials 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 MGCD265, MGCD290 or mocetinostat (MGCD0103); the ability to scale up, formulate and manufacture sufficient GMP, clinical or commercialization quantities of MGCD265, MGCD290 or mocetinostat, 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, MGCD290 or mocetinostat. 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 for the fiscal year ending December 31, 2009, 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 is under no obligation to revise such statements as a result of any event, circumstance or otherwise except in accordance with law.