EntreMed's ENMD-981693 inhibits both Aurora B and Tyr kinase

US drugmaker EntreMed presented encouraging preclinical data on its multi-target kinase inhibitor, ENMD-981693, at the 48th annual meeting of the American Society of Hematology, held in Orlando, Florida. According to the firm, the agent has a unique selectivity profile and multiple mechanisms of action, including antiproliferative activity and the inhibition of angiogenesis. The firm says it is currently conducting studies on this compound, which will enable it to file an Investigational New Drug application with US regulators next year.

In preclinical studies, the agent inhibited a unique profile of tyrosine kinase targets, in addition to the Aurora kinases. ENMD-981693 is selective for Aurora A versus Aurora B. Aurora kinases are key regulators of the process of mitosis or cell division, and are often over-expressed in human cancers. EntreMed noted that ENMD-981693 has shown highly potent activity against oncogenic receptor tyrosine kinases and cytoplasmic tyrosine kinases in vitro, and induces cell cycle arrest and apoptosis in a wide variety of cell lines.