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Methylgene Presents Preclinical Data for Its Multi-targeted (C-Met) Kinase Inhibitor, Mgcd265, at AACR Annual Meeting

Preclinical Data Supports the Potential of the Compound

MONTREAL, Quebec, April 16, 2008 - MethylGene Inc. (TSX:MYG) today disclosed preclinical data for MGCD265, an oral, multi-targeted (c-Met) kinase inhibitor for cancer that targets the c-Met, Tie-2, Ron and VEGF receptor tyrosine kinases. The data were presented in a poster session at the American Association for Cancer Research (AACR) Annual Meeting in San Diego.

In a poster entitled "Preclinical Development of MGCD265, a Potent Orally Active c-Met / VEGFR Multi-targeted Kinase Inhibitor," (poster #4838), results from in vivo human tumor models in mice demonstrated significant inhibition of tumor growth in a broad range of cancer types. In c-Met driven gastric cancer and glioblastoma tumor models, MGCD265 decreased tumor volume by more than 95 percent compared to untreated tumors. Furthermore, MGCD265 showed anti-tumor activity in breast, colorectal and non-small cell lung cancer tumor models that were not c-Met driven, with an average reduction in tumor volume of 76 percent. MGCD265 potently inhibited c-Met and VEGFR2 cellular phenotypes, including cell motility and angiogenesis. Biomarker analysis revealed potent inhibition of in vivo c-Met signal transduction activity and inhibition of downstream Erk and Akt signaling pathways.

MethylGene expects to commence a dose-escalating, Phase I clinical trial (Trial 102) for this compound in solid tumor cancers in April 2008, followed by a second Phase I trial in the second quarter of 2008.

About MGCD265

MGCD265 is an oral, small molecule, multi-targeted kinase inhibitor that targets the c-met, VEGFR1, VEGFR2, VEGFR3, Tie-2 and Ron receptor tyrosine kinases. These receptors appear to play key roles in tumor development and survival, as well as the inappropriate formation of blood vessels (angiogenesis) that nourish the tumor. The kinase inhibition profile of MGCD265 distinguishes it from other agents that specifically target either c-Met or VEGFRs alone.

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 lead product, MGCD0103, is an oral isoform-selective HDAC inhibitor presently in multiple clinical trials for solid tumors and hematological malignancies, including Phase II monotherapy and Phase I, Phase I/II and Phase II combination trials with Vidaza(R), Gemzar(R) and Taxotere(R). MGCD265 is an oral, multi-targeted kinase inhibitor targeting the c-Met, Tie-2, Ron and VEGF receptor tyrosine kinases and the initial Phase I clinical trial is expected to commence in April 2008. In addition, MethylGene's preclinical programs include: MGCD290, an HDAC inhibitor in combination with azoles for fungal infections, a kinase inhibitor program for ocular diseases, and a sirtuin inhibitor program for cancer. MethylGene's development and commercialization partners include Celgene Corporation, Otsuka Pharmaceutical Co. Ltd., Taiho Pharmaceutical and EnVivo Pharmaceuticals. Please visit our website at  .


Eric Goldman

Rx Communications Group


Posted: April 2008