MethylGene Closes Substantial Private Placement

MethylGene Inc. recently announced it has completed its previously announced private placement of 179,690,970 units at a subscription price per unit of Cdn.$0.145 (the Subscription Price), each unit consisting of one common share and thirty one-hundredths (0.30) of a common share purchase warrant, exercisable until November 19, 2017, at an exercise price of Cdn.$0.174 (being 120% of the Subscription Price), for gross proceeds to MethylGene of approximately Cdn.$26.1 million.

The lead investor in the Offering was Tavistock Life Sciences, an insider of the Company, and other insiders participating in the Offering included funds managed by Baker Bros. Advisors, LLC, a fund managed by OrbiMed Advisors LLC, and Tang Capital Partners, LP. Other investors participating in the Offering included RA Capital Management and BVF Partners L.P.

“This funding represents the continuing commitment of our existing shareholders as well as a broadening of our shareholder base,” said Dr. Charles Baum, President and Chief Executive Officer. “The net proceeds from the Offering will enable us to reach significant milestones in our two lead programs, MGCD265 and MGCD290, in 2013 and 2014.”

MGCD265, a multi-targeted receptor kinase inhibitor for oncology, continues to progress and is expected to advance into multiple Phase I/II expansion cohorts upon reaching the Maximum Tolerated Dose (MTD). Indications of interest include renal cell, gastric, hepatocellular, and non-small cell lung (NSCLC) cancers that express the c-Met target. Plans are underway to incorporate the novel target, Axl, into future studies. Axl is elevated in a number of cancer types, including NSCLC, where it is thought to play a role in resistance to EGFR inhibitors. Planning has also commenced for later-stage randomized trials to evaluate MGCD265 in gastroesophageal cancer or NSCLC patients whose tumors express the c-Met target. Additional pilot studies may also be initiated in selected patient populations.

MGCD290, a novel antifungal agent targeting the fungal Hos2 enzyme, will complete enrollment in a randomized, double-blind, placebo-controlled Phase II study in patients with moderate-to-severe vulvovaginal candidiasis (VVC) this quarter, and topline results from this trial will be reported in the first quarter of 2013. Planning is underway for continued development of this agent in VVC, and for expanded development in additional indications including systemic candidiasis.

With the proceeds from the Offering, and based on its current clinical development and operating plans, the Company’s cash runway is expected to extend into the second half of 2014. Jefferies & Company, Inc. and MTS Securities, LLC acted as financial advisors to MethylGene for the Offering in the United States.

MGCD265 is a rationally designed, orally administered small molecule kinase inhibitor that targets the receptor tyrosine kinases (RTKs) Met, VEGFR 1,2,3 and Axl, as well as Tie2 and Ron. RTKs 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, renal, hepatocellular, and ovarian cancers. Phase I/II studies of single agent MGCD265 and combinations with erlotinib or docetaxel are currently underway. More than 200 patients have been treated to date in clinical studies of both single-agent and combination therapy with docetaxel or erlotinib.

MGCD290 is a first-in-class, orally available, small molecule inhibitor of the fungal enzyme Hos2. In preclinical models, the combination with azole antifungal agents results in broader coverage of fungal pathogens and decreases resistance to the most widely used antifungal agents. MGCD290 is being developed as a combination product with fluconazole, the most widely used triazole antifungal. In vitro, MGCD290 in combination with fluconazole reverses fluconazole resistance (primary and acquired) in a wide range of fungal species, including Candida glabrata. MGCD290 has completed multiple Phase I studies in healthy adult volunteers and has shown an excellent safety profile without drug-drug interactions in combination with fluconazole. A randomized, controlled Phase II study in moderate-to-severe VVC is underway.

MethylGene Inc. (MYG.TO) is a drug development company that is advancing novel therapeutics for cancer and infectious disease in human clinical trials. MethylGene owns all rights to its aforementioned lead product candidates, and has partnerships with Otsuka Pharmaceutical Co. Ltd., Taiho Pharmaceutical Co. Ltd., and EnVivo Pharmaceuticals, Inc. for its other pipeline programs. For more information, visit www.methylgene.com.