Research has recently implicated the Aurora kinase family as key mitotic regulators required for genome stability. The kinases Aurora-A, -B and -C are frequently over-expressed in human tumors and appear to be involved in multiple steps of mitosis. Amplification of Aurora-A indicates its importance for tumor formation or progression. Aurora-A has also been identified as an oncogene, transforming cells in vitro. Aurora-B plays a key role in chromosomal alignment and segregation. As such, there exists ample scientific rationale that the inhibition of Aurora kinase is a viable therapeutic approach for the treatment of various cancers.
Using its Translational Technology, TransTech Pharma (TTP) has identified a potent Aurora kinase inhibitor, TTP607 that is a pan-acting selective inhibitor of the Aurora kinase A, B, and C enzymes. TTP607 is reversible and competitive with respect to ATP substrate. TTP607 is a potent inhibitor of Aurora kinase activity and results in inhibition of the growth of various tumor cell line models. More importantly, in vivo results demonstrated antitumor activity of TTP607 in nude or SCID mouse xenograft models of human pancreatic, prostate, breast and colon cancer with no effect on body weight. Efficacy was demonstrated in single and combination drug therapy regimens using various schedules of administration.
Preparation for IND filing is ongoing.