MONTREAL, CANADA -- (Marketwired) -- 04/08/13 -- MethylGene Inc. (TSX: MYG) today announced that preclinical data for the kinase inhibitor MG516 was presented at the American Association for Cancer Research (AACR) Annual Meeting held in Washington DC. In a poster entitled "Preclinical characterization of MG516, a novel inhibitor of receptor tyrosine kinases involved in resistance to targeted therapies" data was presented showing that MG516 possesses potent inhibitory activity against a spectrum of tyrosine kinase receptor targets including Eph receptors and Ret as well as Met, Axl and VEGF-R family members. The study incorporated data from in vitro kinase and cell-based analyses. In a broad variety of animal models of human cancer, MG516 demonstrated significant inhibition of tumor growth accompanied by suppression of the target kinases. MG516 also reversed resistance to the VEGFR inhibitor sunitinib in an in vivo preclinical tumor model.
"MG516 inhibits a novel spectrum of targets that have been shown to be drivers of tumor growth" said Dr. Charles Baum, President and Chief Executive Officer of MethylGene Inc. "This molecule is a valuable addition to MethylGene's oncology portfolio that is complementary to our MGCD265 program and has the potential to address unmet needs in patients with cancer".
MG516 is a multi-targeted kinase inhibitor that covers a novel spectrum of targets including members of the Eph receptor family, the Met receptor, the Ret receptor tyrosine kinase, and all three vascular endothelial growth factor receptors (VEGFR 1, 2, 3). Eph is over-expressed in several cancers including gastric, breast, prostate and esophageal and is associated with resistance to HER2 inhibitors. Ret is expressed and has a role in medullary thyroid carcinoma, and recent data suggest a possible role as a driver of growth in lung cancer. MG516 has demonstrated potent inhibition of kinases in vitro, in multiple cell-based assays and has shown up to 100% of tumor growth inhibition in vivo against a number of tumor types in xenograft studies. In preclinical models anti-tumor activity is achieved at low doses and MG516 is well tolerated without significant weight loss or myelosuppression. MG516 is in advanced preclinical development and ready to commence IND-enabling studies.
MethylGene Inc. (TSX: MYG) is a drug development company that is advancing novel therapeutics for the treatment of patients with cancer and infectious disease in human clinical trials. The Company's lead clinical stage product candidates are: MGCD265, a multi-targeted receptor tyrosine kinase inhibitor that is in Phase I/II clinical trials for patients with solid tumors and MGCD290, an oral antifungal agent targeting the fungal Hos2 enzyme that was in Phase II trials for vulvovaginal candidiasis. 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.
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