In addition to our lead kinase inhibitor MGCD265, MethylGene has developed a novel multi-targeted kinase inhibitor, MG91516, that demonstrated potent inhibition of enzymatic activities in vitro and in multiple cell-based assays and in a broad spectrum of xenograft studies. The profile of MG91516 features the inhibition of a novel spectrum of targets which include members of the Eph receptor family, the Ret receptor tyrosine kinase, Met, and all three vascular endothelial growth factor receptors (VEGFR 1, 2, 3).

The inclusion of Eph and Ret as targets is important due to their overexpression and/or mutation in a number of cancers. Eph is overexpressed in several cancers including gastric, lung, breast, ovarian, brain and skin while the activating mutations of Ret are primarily associated with medullary thyroid carcinoma (MTC).

MG91516 is in advanced preclinical development and ready to commence IND-enabling studies.