METHYLGENE REPORTS FAVORABLE PRELIMINARY PHASE I DATA FOR MGCD265,
ITS MULTI-TARGETED (C-MET) KINASE INHIBITOR, AT ASCO ANNUAL MEETING

·          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

Montreal, Quebec. May 28, 2009 – 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.

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