Highlights 

• Rachel W. Humphrey, MD was appointed as Executive Vice President and Chief Medical Officer on January 4, 2012.
• During this quarter, we strengthened our Board of Directors with the appointments of Henry J. Fuchs MD and Peggy Mulligan FCA.
• Our MGCD290 Phase II clinical trial and MGCD265 Phase I/II clinical trials continued to enroll patients.
• Preclinical data from our MGCD265 oncology program was presented at the American Association for Cancer Research Annual Meeting.
• In May 2012, we opened our US office in Princeton, New Jersey.
• We finished the quarter with $25.1 million in cash and cash equivalents.

“MethylGene continued to make solid progress in this quarter,” said Charles Grubsztajn, President and CEO of MethylGene. “The clinical programs for both MGCD290 and MGCD265 continue to progress, and we made key additions to our management team and Board of Directors to ensure that we have the optimal balance of skills and experience to lead us through the next steps.”

First Quarter 2012 Financial Results Reported in Canadian Dollars

Click here to view the Q1 press release with financial statements.

The Company’s financial statements for the period ended March 31, 2012 have been prepared in accordance with IAS 34, Interim Financial Reporting, as issued by the International Accounting Standards Board (IASB).

We had minimal revenues in the first quarter ended March 31, 2012 compared to $1.3 million for the first quarter of 2011, as the research component of the agreement with Otsuka Pharmaceutical Co. Ltd. ended in June 2011 and we had fully amortized the remaining deferred revenues for both Otsuka and Taiho Pharmaceutical Co. Ltd. in the second and fourth quarters of 2011, respectively.

Research and development expenditures, net of investment tax credits, for the first quarter of 2012 were $2.2 million compared to $1.8 million for the first quarter of 2011. This increase is due to increased clinical development activity with both the MGCD290 and MGCD265 programs, increased compensation costs with the appointment of the Chief Medical Officer and was partly offset by higher investment tax credits.

General and administrative expenses in the first quarter of 2012 were $1.2 million compared to $1.0 million in the first quarter of 2011.  This primarily relates to higher non-cash stock option expenses.

Financial income of $69,000, relating primarily to interest income, in the first quarter of 2012 was $62,000 higher compared to the first quarter of 2011 due to increased cash balances versus the prior year. The Company recorded a foreign exchange gain of nil in the first quarter of 2012 compared to a loss of $11,000 in the first quarter of 2011.

The net loss and comprehensive loss for the first quarter ended March 31, 2012 was $3.4 million, or ($0.01) per share, compared to a net loss and comprehensive loss of $1.6 million, or ($0.04) per share, for the same period last year. The decreased loss per share relates to the higher number of shares outstanding at the end of the first quarter 2012 versus the first quarter of 2011.

Cash, cash equivalents, marketable securities and restricted cash totaled $25.1 million as at March 31, 2012 compared to $29.6 million on December 31, 2011. The Company believes it has sufficient financial resources to carry forward its current clinical development and operating plans into the fourth quarter of 2013.

MGCD290 Clinical Development Update

MGCD290 is a first-in-class, selective, oral small molecule inhibitor of the fungal enzyme Hos2, initially being developed in combination with fluconazole, the most widely used triazole antifungal. We recently commenced a randomized controlled phase II trial of MGCD290 in moderate to severe acute vulvovaginal candidiasis (VVC), a form of yeast infection for which there is only limited response from standard treatments. This trial will assess the effectiveness of MGCD290 in combination with fluconazole, as compared to fluconazole alone.  Initially, a higher than expected number of patients were ineligible at screening, leading us to amend the protocol and add additional sites in order to accelerate recruitment. We expect that most of the new sites will be open under the new protocol this quarter. We continue to expect to report topline data from this trial around year end 2012. We are also planning to initiate a second randomized trial in VVC. We completed a fifth phase I study in the first quarter of 2012 to assess the effect of food on MGCD290 bioavailability, as well as to evaluate its distribution to clinically relevant tissues. The study has been completed and no serious adverse events were reported. The data suggest food increased exposure and that MGCD290 was present in clinically relevant tissues. The data from this trial will be used to guide future studies.

MGCD265 Clinical Development Update

MGCD265 is a rationally designed, orally available kinase inhibitor targeting a unique spectrum of RTKs including Met, VEGFR 1, 2, and 3, RON and Tie-2. We continue to enroll patients in MGCD265 phase  I/II monotherapy trials and combination trials with erlotinib or docetaxel and as of April 30, 2012 over 198 patients have been treated in these trials. We also recently completed a food effect study with MGCD265. Preliminary results from this study suggest that combining MGCD265 with food improves exposure to the drug and we have incorporated this into our ongoing trials. Our development plan for MGCD265 is to expand the monotherapy and combination therapy trials with selected cohorts of tumor types once the maximum tolerated dose is reached. The data from the expansion cohorts will be used to guide randomized phase II studies.

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 solid tumor cancers. 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.

Montreal, Canada. April 2, 2012 – MethylGene Inc. (TSX:MYG) today disclosed preclinical data during a presentation for its proprietary multi-targeted kinase inhibitor, MGCD265, at the 2012 AACR Annual Meeting held in Chicago, Illinois.

Results were presented showing the potent inhibition of tumor growth by the combination of MGCD265 with erlotinib and providing additional support to the mechanisms underlying this anti-tumor effect. This combination was more effective than either erlotinib alone or MGCD265 alone resulting in tumor regression in a pre-clinical model of gastric cancer. Gene expression analysis revealed that pathways impacted by this drug combination included inhibition of cell growth, induction of apoptosis and regulation of glycolysis. The expression of glycolysis-regulating genes was partly downregulated by either MGCD265 or erlotinib alone. However, the combination led to a significant depression of regulators of glycolysis, including the key mediator hexokinase 2 (HK2). The poster is entitled  “The Combination of MGCD265, a Met/VEGFR Inhibitor in Clinical Development, and Erlotinib Potently Inhibits Tumor Growth by Altering Multiple Pathways Including Glycolysis,” (abstract no. 1790).

The observation that the glycolysis pathway is inhibited by the combination of MGCD265 with erlotinib reinforces the rationale of combining MGCD265 with EGFR inhibitors in clinical trials. The ability of cancer cells to alter their metabolism in order to grow more rapidly has been recognized for many years. The expression and activity of enzymes in the glycolysis pathway is modified to allow for uncontrolled growth of the tumor. This pathway has recently emerged as an interesting target for oncology drug development.

These results support the ongoing clinical development of MGCD265 in combination with EGFR inhibitors as an anti-cancer therapy. Early results from clinical trials investigating MGCD265 in combination with erlotinib have demonstrated encouraging signs of activity in gastric cancer patients. An update on clinical activities of MGCD265 is anticipated at a future medical meeting.

Science Policy Session

In a separate Science Policy session at the AACR meeting: “Scientific and Regulatory Challenges in Codevelopment of Predictive In Vitro Diagnostics”, Dr. Rachel Humphrey, Chief Medical Officer of MethylGene Inc., will give an oral presentation entitled “Biomarkers in clinical development: Strategic considerations”. The presentation will be held at McCormick Place South (Level 1), Room S103.

About MGCD265

MGCD265 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 completed one Phase 1 single agent study, and is nearing completion of one Phase 1 single agent clinical trial and two Phase 1/2 combinations, one with docetaxel and one with erlotinib 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 2 trials for vulvovaginal candidiasis and MGCD265, an oral Met/VEGF receptor kinase inhibitor that is in Phase 1/2 clinical trials for solid tumor cancers. 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.

In another session on science policy, MethylGene’s Chief Medical Officer, Dr. Rachel Humphrey, will give a presentation on the use of biomarkers in clinical development.

Poster Presentation

The Combination of MGCD265, a Met/VEGFR Inhibitor in Clinical Development, and Erlotinib Potently Inhibits Tumor Growth by Altering Multiple Pathways Including Glycolysis

Date and Time: Monday Apr 2, 2012 8:00 AM – 12:00 PM (CT)
Session:  Experimental and Molecular Therapeutics 11
Abstract No.: 1790
Location: Hall F, Poster Section 29

Science Policy Session

Dr. Humphrey’s presentation is entitled “Biomarkers in clinical development: Strategic considerations”.

Date and Time: Monday Apr 2, 2012 1:30 – 1:50 PM (CT)
Session: SP03. Scientific and Regulatory Challenges in Codevelopment of Predictive In Vitro Diagnostics
Location: McCormick Place South (Level 1), Room S103

About MGCD265

MGCD265 is a novel, oral 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 completed one Phase 1 single agent study, and is nearing completion of one Phase 1 single agent clinical trial and one Phase 1/2 combination clinical trial (with erlotinib and 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 2 trials for vulvovaginal candidiasis, and MGCD265, an oral Met/VEGF receptor kinase inhibitor that is in Phase 1/2 clinical trials for solid tumor cancers. 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.

“Peggy is a financial and audit expert, and a well respected business leader. We look forward to her guidance as we plan for the future”, said Charles Grubsztajn, President and CEO of MethylGene.

Peggy most recently served as Executive Vice President and Chief Financial Officer of Valeant Pharmaceuticals International, Inc (formerly Biovail Corporation), a multinational pharmaceutical company listed on both the New York Stock Exchange and Toronto Stock Exchange. During her tenure, she co-led the merger and subsequent integration with Valeant Pharmaceuticals International, Inc. She is currently a member of the Board of Directors of Ontario Power Generation Inc. (“OPG”) and Chair of OPG’s Human Resources & Compensation Committee. From 2005 to 2007 Peggy served as Executive Vice President, Chief Financial Officer and Treasurer of Linamar Corporation. Previously Peggy spent eleven years in various roles at the Bank of Nova Scotia, most recently as Executive Vice President, Systems & Operations. Before joining the Bank of Nova Scotia she was an Audit Partner with Price Waterhouse. In 2003 and 2004 Ms. Mulligan was named one of Canada’s Top 100 Most Powerful Women by the Women’s Executive Network.

She holds a B. Math (Honours) from the University of Waterloo and she is a Fellow of the Institute of Chartered Accountants (FCA) of Ontario.

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 2 trials for vulvovaginal candidiasis and MGCD265, an oral Met/VEGF receptor kinase inhibitor that is in Phase 1/2 clinical trials for solid tumor cancers. 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.

Highlights

• During the fourth quarter we commenced our first randomized, controlled Phase 2 study with MGCD290, and our two Phase 1 dose escalation studies with MGCD265 continued to enroll patients.
• On January 4^th, 2012 we strengthened our management team with the appointment of Rachel Humphrey, MD as Executive Vice President and Chief Medical Officer.
• On November 13^th, 2011 we reported final results for MGCD265 Trial 265-102 at the 2011 AACR-NCI-EORTC Molecular Targets and Cancer Therapeutics Conference.
• We finished the quarter with over $29 million in cash and equivalents to fund our development programs.

“Last year was a very successful year for MethylGene,” said Charles Grubsztajn, President and CEO of MethylGene. “In 2011 we raised $34.5 million from thought-leading investors, made key additions to our management team and Board of Directors, reported data on MGCD265 at ASCO in June, and commenced a randomized, controlled Phase 2 trial with our first-in-class antifungal agent MGCD290. We expect continued clinical progress, and to report additional clinical data, in 2012.”

International Financial Reporting Standards

The financial statements of the Company for the year ended December 31, 2011, have been prepared for the first time in accordance with International Financial Reporting Standards (IFRS) as issued by the International Accounting Standards Board (IASB). They have been prepared: on a historical cost basis, except for financial instruments that have been measured at fair value; in accordance with IAS 1, Presentation of Financial Statements; in accordance with IFRS 1, First-time Adoption of IFRS; and in accordance with IFRS standards and IFRIC interpretations issued and effective or issued and early adopted as at the time of preparing these statements.

Fourth Quarter 2011 Financial Results Reported in Canadian Dollars

Click here to view Q4 press release with financial statements.

Revenues for the fourth quarter of 2011 of $468,000 were $348,000 lower versus the fourth quarter of 2010 due to lower research collaborations and contract revenues from Otsuka Pharmaceutical Co. Ltd. (“Otsuka”), as the research component of our collaboration agreement ended in June 2011.

Research and development expenditures, net of investment tax credits, for the fourth quarter of 2011 were $3.1 million compared to $1.9 million for the fourth quarter of 2010. This increase is mainly due to higher compensation and third-party clinical costs as we increased clinical development activities related to both of our lead programs, MGCD290 and MGCD265. These increases were partially offset by lower lease-related costs.

General and administrative expenses in the fourth quarter of 2011 were $1.0 million compared to $879,000 in the fourth quarter of 2010. This increase relates to higher compensation costs partially offset by lower professional fees.

Financial income of $82,000, relating primarily to interest income, in the fourth quarter of 2011 was $67,000 higher compared to the fourth quarter of 2010 due to increased cash balances and higher average interest rates versus the prior year. The Company recorded a foreign exchange loss of $9,000 in the fourth quarter of 2011 versus a loss of $17,000 in the fourth quarter of 2010.

The net loss and comprehensive loss for the fourth quarter of 2011 was $3.6 million, or ($0.01) per share, versus a net loss and comprehensive loss of $2.0 million or ($0.05) per share for the same period last year. The improved loss per share relates to the higher average number of shares outstanding at the respective quarter ends, partially offset by the higher loss in the fourth quarter of 2011 compared to the fourth quarter of 2010.

Full Year 2011 Financial Results in Canadian Dollars

Revenues for 2011 of $3.1 million were $703,000 higher versus 2010, as higher license and up-front fees from Otsuka and Taiho Pharmaceutical Co. Ltd. offset lower research collaborations and contract revenues from Otsuka as the research component of the collaboration agreement ended in June 2011. 

Research and development expenditures, net of investment tax credits, for 2011 were $8.8 million versus $10.9 million for 2010. This decrease is mainly due to lower lease-related costs and lower compensation costs. Third-party clinical development costs in connection with our lead programs MGCD290 and MGCD265 were marginally higher in 2011 as compared to 2010.

General and administrative expenses in 2011 were $4.3 million versus $6.1 million in 2010.  This decrease relates primarily to the one-time costs of $1.5 million associated with the departure of the previous CEO in 2010, which was partially offset by higher non-cash stock option expenses in 2011.

Financial income of $262,000 for 2011, relating primarily to interest income, was $238,000 higher versus 2010 due to increased cash balances and higher average interest rates versus the prior year. The Company recorded a foreign exchange gain of $42,000 in 2011 compared to a loss of $72,000 in 2010.

The net loss and comprehensive loss for 2011 was $9.7 million, or ($0.04) per share, versus a net loss and comprehensive loss of $14.7 million or ($0.36) per share for the same period last year. The improved loss per share relates to the higher average number of shares outstanding at the respective year ends and the lower loss in 2011 compared to 2010. 

Cash, cash equivalents, marketable securities and restricted cash totaled $29.6 million as at December 31, 2011 compared to $8.6 million as at December 31, 2010. Due to increased clinical activity, the Company believes it has sufficient financial resources to carry forward its current clinical development and operating plans only into the fourth quarter of 2013.

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 2 trials for vulvovaginal candidiasis and MGCD265, an oral Met/VEGF receptor kinase inhibitor that is in Phase 1/2 clinical trials for solid tumor cancers. 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.

Mr. Grubsztajn’s presentation will be available live via webcast at www.methylgene.com.

About MethylGene

MethylGene Inc. (TSX:MYG) 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 will start randomized Phase 2 trials in the near term. The Company’s partners include Otsuka Pharmaceutical Co. Ltd., Taiho Pharmaceutical Co. Ltd., and EnVivo Pharmaceuticals, Inc.

“Dr. Fuchs is a highly regarded leader in the biotechnology industry and brings a wealth of drug development and management experience at public life science companies. We look forward to his contributions as we advance our key clinical programs,” said Charles Grubsztajn, President and CEO of MethylGene.

Henry Fuchs, MD is currently Executive Vice President and Chief Medical Officer of BioMarin Pharmaceutical Inc. (NASDAQ: BMRN), and is a seasoned biotech drug development executive. From 2005 to 2009, Dr. Fuchs was Executive Vice President and Chief Medical Officer of Onyx Pharmaceuticals (NASDAQ: ONXX), overseeing expanded development of the kinase inhibitor Nexavar and other key development programs. From 1996 to 2005, Dr. Fuchs served in multiple roles of increasing responsibility at Ardea Biosciences (NASDAQ: RDEA), first as Vice President, Clinical Affairs, then as President and Chief Operating Officer, and finally as Chief Executive Officer. From 1987 to 1996, Dr. Fuchs held various positions at Genentech where, among other responsibilities, he led the clinical program that resulted in the approval of Pulmozyme. Dr. Fuchs was also responsible for the Phase III development program that led to the approval of Herceptin to treat metastatic breast cancer.

Dr. Fuchs received an M.D. degree from George Washington University and a B.A. degree in biochemical sciences from Harvard University.

About MethylGene

MethylGene Inc. (TSX:MYG) 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 will start randomized Phase 2 trials in the near term. The Company’s partners include Otsuka Pharmaceutical Co. Ltd., Taiho Pharmaceutical Co. Ltd., and EnVivo Pharmaceuticals, Inc.

“Dr. Humphrey brings a wealth of drug development experience to MethylGene, and we look forward to her actively guiding our clinical development programs, particularly MGCD265 for the treatment of cancer and MGCD290 for the treatment of fungal diseases,” said Charles Grubsztajn, President and CEO of MethylGene.

Dr. Humphrey joins MethylGene from Bristol-Myers Squibb (NYSE: BMY), where she was most recently Vice President, Global Development Lead, Immuno-Oncology. From 2003 to 2011, Dr. Humphrey supervised a number of in-licensed and internal development programs including  the Phase II – IV development of ipilimumab (YERVOY®), which achieved global approval for the treatment of metastatic melanoma in 2011. From 1997 until 2003 Dr. Humphrey held increasingly senior clinical development positions at Bayer (XETRA: BAYN), leading the IND filing and the development of the multiple kinase inhibitor sorafenib (Nexavar®), which subsequently achieved global approval for advanced renal cell carcinoma and hepatocellular carcinoma.

Dr. Humphrey received her B.A. degree in biochemistry from Harvard University, her M.D. degree from Case Western Reserve University, and completed her Medical Residency at the Johns Hopkins Hospital. From 1992 until 1997 Dr. Humphrey worked at the U.S. National Cancer Institute (NCI), first as a Clinical Oncology Fellow and later as a Staff Physician/Scientist in the NCI’s HIV and AIDS Malignancy Branch.

About MethylGene

MethylGene Inc. (TSX:MYG) 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 will start randomized Phase 2 trials in the near term. The Company’s partners include Otsuka Pharmaceutical Co. Ltd., Taiho Pharmaceutical Co. Ltd., and EnVivo Pharmaceuticals, Inc.

http://www.corporate-ir.net/ireye/confLobby.zhtml?ticker=MYG.TO&item_id=4674204.

 About MethylGene

MethylGene Inc. (TSX:MYG) 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 and will start randomized Phase 2 trials in the near term. The Company’s partners include Otsuka Pharmaceutical Co. Ltd., Taiho Pharmaceutical Co. Ltd., and EnVivo Pharmaceuticals, Inc.

“We are pleased that MGCD265, when dosed in an intermittent (week on, week off) schedule, was very tolerable for patients and showed early signs of clinical benefit,” commented Dr. Jeff Besterman, Chief Scientific Officer of MethylGene. “The excellent tolerability of MGCD265 in this intermittent schedule was consistent with the continuous dose regimens used in Trials 265-101 and 265-103. We continue to enroll patients in Trials 265-101 and 265-103, and we will report additional data from these ongoing studies in 2012.”

Poster Session

“The Determination of the Maximum Tolerated Dose (MTD) of MGCD265 on an Intermittent Schedule: Phase I Study Results (Study 265-102)” Abstract #A95. (Click on title to access pdf version)

Forty-seven patients were enrolled in this Phase 1, open-label, dose-escalation study to evaluate the safety and MTD of oral MGCD265 as a single agent when dosed intermittently. MGCD265 was administered daily (one week on, one week off) to patients with a variety of advanced solid malignancies for 28–day cycles. There were no treatment-related serious adverse events (SAEs). The most frequent treatment-related adverse events were diarrhea, fatigue and nausea, and most were of modest severity (grade 1 or 2). Dose-limiting toxicities were grade 3 mood alteration and grade 3 fatigue in one patient, and grade 3 hemoptysis in another patient. The MTD in this single agent study was determined to be 128 mg/m² twice daily (BID). In this group of patients with advanced disease treated with MGCD265, 4 had prolonged stable disease (6-14 cycles).

About MGCD265

MGCD265 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 Target

The 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 MethylGene

MethylGene Inc. (TSX:MYG) 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 and will start randomized Phase 2 trials in the near term. The Company’s partners include Otsuka Pharmaceutical Co. Ltd., Taiho Pharmaceutical Co. Ltd., and EnVivo Pharmaceuticals, Inc.