MethylGene Reports Favorable Preliminary Phase I Data for MGCD265, Its Multi-Targeted (c-Met) Kinase Inhibitor, at ASCO Annual Meeting

MONTREAL, QUEBEC--(Marketwire - May 28, 2009) - MethylGene Inc. (TSX: MYG)

- Compound is well tolerated with early signs of activity at doses tested to date

- Phase I dose escalation continues

- Phase II program expected to commence in third quarter of 2009 focused on non-small cell lung cancer patients

MethylGene Inc. (TSX: MYG) today reported preliminary Phase I data for MGCD265, an oral, multi-targeted kinase inhibitor for cancer that targets the c-Met, VEGF, Ron and Tie-2 receptor tyrosine kinases. Preliminary data from the two clinical trials (Trials 102 and 101) evaluating the compound in solid tumors were published in the proceedings from the American Society of Clinical Oncology’s (ASCO) annual meeting. The abstracts with additional updated information describe the favorable safety profile and early signs of activity at doses tested.

The objectives of the two Phase I dose-escalation trials were to evaluate the safety, pharmacodynamics (PD) and pharmacokinetics (PK) of MGCD265 when administered orally to patients with advanced metastatic or unresectable solid tumors that were refractory to standard therapy. The starting dose for both trials was 24mg/m2. In Trial 102, MGCD265 is administered daily every other week over a 28-day cycle, whereas in Trial 101, MGCD265 is administered daily on a continuous basis over a 21-day cycle.

Preliminary results from Phase I Trials

MGCD265 demonstrated early signs of activity at doses tested and a favorable safety profile.

To date, 16 patients have been enrolled in Trial 102 and 14 patients in Trial 101. Patients received doses of MGCD265 ranging from 24 mg/m2 to 255 mg/m2 with the maximum tolerated dose still being investigated. No dose-limiting toxicities have been observed.

In Trial 102, 12 patients have been evaluated for efficacy at dose levels of 24, 48, 96 and 192 mg/m2. Of these patients, five experienced stable disease per RECIST criteria, including one patient with aggressive bladder cancer who remains on MGCD265 treatment after ten cycles and a medullary thyroid cancer patient who experienced tumor shrinkage. Interestingly, an archived tumor biopsy obtained prior to MGCD265 treatment from the patient with aggressive bladder cancer shows c-Met expression and phosphorylation. In Trial 101, ten patients have been evaluated for efficacy at dose levels of 24, 48, 96 and 150 mg/m2. Two of these patients experienced stable disease per RECIST criteria.

Across both studies, MGCD265 appears to have a good safety profile at the doses administered with only four drug-related grade two adverse events and no grade three or higher drug-related adverse events in the 26 patients evaluated for safety. The most frequently reported drug-related grade two adverse event was diarrhea.

The compound also demonstrated encouraging PD changes in the VEGF, HGF and shed c-Met plasma markers. The preliminary PK findings for MGCD265 also indicated a dose-dependent increase in exposure with a mean half-life of approximately 26 hours.

“We are pleased with the overall safety and pharmacokinetic data compiled to date, as well as the early signs of activity in several of the treated patients,” said Donald F. Corcoran, President and Chief Executive Officer of MethylGene. “Our goal is to begin our Phase II program with a Phase I/II combination trial with Tarceva® or Taxotere® in the third quarter of 2009 as MGCD265’s mechanism of action appears to synergize with these anticancer agents.”

MethylGene will continue to dose escalate in the two ongoing Phase I trials and commence a Phase II program with the initiation of a randomized Phase I/II combination trial with MGCD265 and Tarceva® or Taxotere® focused on non-small cell lung cancer (NSCLC) patients. MethylGene has demonstrated preclinical synergistic in vivo efficacy and tolerability of MGCD265 in combination with both agents. The Tarceva® combination is of particular interest, since it has been shown that c-Met and EGFR functionally cooperate. The simultaneous inhibition of c-Met and EGFR has demonstrated enhanced anti-tumor activities in multiple in vivo models. Importantly, c-Met amplification has been described as a mechanism of resistance to EGFR inhibitors in NSCLC patients; therefore, blocking c-Met offers a compelling rationale to overcome resistance to EGFR inhibitors in the clinic.

About MethylGene

MethylGene Inc. (TSX: MYG) is a publicly-traded, clinical stage, biopharmaceutical company focused on the discovery, development and commercialization of novel therapeutics for 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 I clinical trials for solid tumor cancers; MGCD290, a fungal Hos2 (HDAC) inhibitor being developed for use in combination with fluconazole for serious fungal infections that is also 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.