MONTREAL, QUEBEC--(Marketwire - June 3, 2011) - MethylGene Inc. (TSX:MYG - News) today disclosed safety and efficacy clinical data for MGCD265, its proprietary oral Met/VEGF receptor tyrosine kinase inhibitor, at the 2011 ASCO Annual Meeting held in Chicago, Illinois. Details will be presented in two poster sessions for the Company's two-arm Phase 1/2 clinical trial (Trial 265-103) in which MGCD265 is administered in combination with either docetaxel or erlotinib in patients with solid tumor cancers.Poster Discussion Session"Determination of the Maximum Tolerated Dose (MTD) of MGCD265, an Oral Met/VEGFR Multi-Targeted Kinase Receptor Tyrosine Kinase Inhibitor, in Combination with Docetaxel." Abstract #3032.In the docetaxel arm of Trial 265-103 (MGCD265 in combination with docetaxel), 24 patients with advanced solid malignancies have been enrolled. MGCD265 was orally administered daily in combination with docetaxel once every 21 days (one cycle). The maximum-tolerated dose (MTD) of MGCD265 has been determined to be 72 mg/m2 twice daily (BID) in combination with full dose docetaxel (75 mg/m2). Of the 24 patients in this combination arm, eight are non-small cell lung cancer (NSCLC) patients. To date, six of the NSCLC patients were on study for more than four cycles with two patients experiencing partial responses (PRs) and three patients experiencing prolonged disease stabilization (on study for approximately 9 to 13 months). One patient is still continuing. Five out of six of these patients with NSCLC were previously exposed to a prior line of therapy containing a taxane. The most frequent treatment-related toxicities grade 2 and above in this combination arm include neutropenia, anorexia, diarrhea and fatigue.Poster Session"MGCD265, an Oral Met/VEGFR Multi-Targeted Receptor Tyrosine Kinase Inhibitor, in Combination with Erlotinib: Phase I Clinical Experience." Abstract #3083.In the erlotinib arm of Trial 265-103 (MGCD265 in combination with erlotinib), 34 patients have been enrolled and dose escalation continues. Both of the agents are administered orally daily to patients with advanced solid malignancies for 21-day cycles. Of the 34 patients in this combination arm, three are patients with gastric cancer. Two of these patients are on study for a prolonged period (greater than eight months). One of these patients with linitis plastica (a form of gastric cancer) experienced complete resolution of ascites and a decrease in gastric wall thickness and is on study for over one year. Molecular profiling of the archived tumor biopsy from this patient showed high levels of Met and phospho-Met protein expression in the absence of MET and EGFR gene amplification or detectable mutations. The most frequent treatment-related toxicities grade 2 and above in this combination arm include diarrhea, rash and fatigue."The preliminary activity seen in NSCLC with MGCD265 in combination with docetaxel, and in gastric cancer with MGCD265 in combination with erlotinib, are exciting. To date, these combinations have been generally well tolerated with predictable safety profiles in our patients," commented Dr. Amita Patnaik, Associate Director of Clinical Research at South Texas Accelerated Research Therapeutics (START) in San Antonio, Texas. "We look forward to conducting additional studies in order to confirm these early signals."About MGCD265MGCD265 is a novel, orally active small molecule inhibitor that targets a unique spectrum of receptor tyrosine kinases: Met, VEGFR 1, 2, and 3, Tie-2 and Ron. These kinases play key roles in tumor development, survival and metastasis as well as the inappropriate formation of blood vessels (angiogenesis) that nourish the tumor. MGCD265 has been well-tolerated, either alone or in combination, and has shown preliminary signs of clinical activity.About the Met TargetThe Met receptor is a protein that is found on the cell's surface. When not properly regulated (i.e. over active) it plays a key role in the growth, survival and metastasis of various types of cancers. Met is also involved in angiogenesis and is strongly associated with major cancers such as non-small cell lung, gastric, prostate and triple negative breast carcinomas.About MethylGeneMethylGene Inc. (TSX:MYG - News) is a clinical-stage biopharmaceutical company that develops novel therapeutics for cancer and infectious disease. The Company's lead product candidates include: MGCD265, an oral Met/VEGF receptor kinase inhibitor that is in Phase 1/2 clinical trials for solid tumor cancers and MGCD290, a fungal Hos2 inhibitor, for use in combination with fluconazole for fungal infections, which has completed Phase 1 clinical studies. The Company's partners include Otsuka Pharmaceutical Co. Ltd., Taiho Pharmaceutical Co. Ltd., and EnVivo Pharmaceuticals, Inc.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, 2010, 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.