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.
Investor Relations Contact:
Joseph Walewicz, CFA
Vice President, Business & Corporate Development
MethylGene Inc.
Phone: 514-337-3333 ext. 373
ir@methylgene.com
www.methylgene.com
Thomas Fechtner
Vice President
The Trout Group LLC
Phone: 646-378-2931
tfechtner@troutgroup.com
www.troutgroup.com
