MONTREAL, QUEBEC--(Marketwire - Oct. 1, 2012) - MethylGene Inc. (TSX:MYG) announced that clinical data from its MGCD265 Met/VEGFR-targeted oncology program were presented today at the European Society for Medical Oncology (ESMO) 2012 Congress, held in Vienna, Austria. Three poster presentations provided updates on the ongoing monotherapy, combination therapy and healthy volunteer trials.

"These data demonstrate the clinical activity of MGCD265 as well as its distinct profile relative to other Met-targeted agents." said Dr. Rachel Humphrey, Executive Vice President and Chief Medical Officer of MethylGene. "The continued favorable safety profile at clinically relevant exposures and the preliminary signs of clinical benefit are encouraging."

The poster entitled "A Phase I, dose-escalation study of MGCD265, a multi-targeted oral tyrosine kinase receptor inhibitor, for treatment of advanced solid tumors" (abstract 471P) documented the safety profile, pharmacokinetics, pharmacodynamics and clinical response observed to date in the ongoing monotherapy Trial 265-101. MGCD265 continues to exhibit a favorable safety profile with drug-related adverse events being mostly mild to moderate. The maximum tolerated dose (MTD) has not yet been reached. Drug-related grade 3 adverse events seen in more than one patient were diarrhea, fatigue and elevated lipase (n=2 for each). Stable disease was achieved in 36% of patients (24/67 patients). No objective responses have been seen to date. Dose-dependent Met inhibition was demonstrated using samples of patient plasma, and drug exposures have reached the range shown to have antitumor effects in animal models.

Data from the ongoing combination Trial 265-103 was presented in the poster entitled "Clinical effects of MGCD265, an oral tyrosine kinase inhibitor, in combination with erlotinib or docetaxel for treatment of advanced gastroesophageal and NSCLC tumors" (abstract 492P). This poster highlighted the clinical responses seen in patients with non-small cell lung cancer (NSCLC, n=12) or gastro-esophageal cancer (GE, n=9) treated with MGCD265 in combination with docetaxel or erlotinib in an ongoing dose-escalating Phase I study. Among twelve patients with NSCLC treated with MGCD265 (up to 600 mg / m²), nine achieved disease control (seven stable disease and two partial responses). Four NSCLC patients were progression-free for 7-11 months. In the GE cohort, five of nine patients treated with MGCD265 (up to 324 mg / m²) achieved disease control (all stable disease). Three of these patients remained stable for 11-22 months, an increase of 6-11 fold compared to the length of time on prior therapy. The safety profile of MGCD265 in combination with docetaxel or erlotinib was acceptable at doses up to 600 mg / day with no apparent increase in frequency of the adverse events that are commonly associated with docetaxel and erlotinib, respectively. Dose escalation is ongoing and the MTD has not been defined for either combination.

The third poster entitled "Pharmacokinetic profile of MGCD265, an oral tyrosine kinase inhibitor, with or without food in healthy volunteers" (abstract 493P) described the recently completed Phase I Trial 265-105 which assessed the effect of food on MGCD265 pharmacokinetics. This study showed that administration of MGCD265 in the presence of food increased drug exposure significantly, with no added toxicity. Based on these findings, food has been incorporated into all ongoing MGCD265 clinical trials.

All three posters are available on our website at [ http://methylgene.com/mgcd265/mgcd265-posters-publications ].

About MGCD265

MGCD265, a rationally designed, orally administered small molecule kinase inhibitor designed to target Met and VEGFR 1,2, and 3 receptor tyrosine kinases (RTKs). RTKs, including Met, are key kinases involved in cancer, angiogenesis (a process whereby new blood vessels are formed to nourish the tumors), tumor cell metastasis, tumor development and survival. Met expression is elevated and associated with tumorigenesis in several solid tumor indications including NSCLC, gastric, prostate, colorectal, bladder, breast and ovarian cancers. Two clinical trials (Phase I and Phase I/II) are ongoing using the agent as a monotherapy and in combination with erlotinib or docetaxel in solid tumors.

About MethylGene

MethylGene Inc. (TSX:MYG) is a small molecule drug development company that is advancing two 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 currently 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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