Cancer remains second only to heart disease as the leading cause of death among Americans.  Moreover, survivors of cancer continue to suffer from symptoms of depression, fatigue and pain, despite treatment advances. While a number of targeted pharmaco-therapies have been developed in the past decade, the advent of new treatment options remains important in the fight against this multi-faceted disease.

It is now well understood that protein kinases play key roles in the growth and survival of cancer cells by regulating their onset of DNA synthesis, their response to DNA damage and their entry, progression, and exit from mitosis.  Clinical validation that protein kinases are an attractive class of therapeutic drug targets for cancer is the recent approval of six protein kinase inhibitors, Gleevec® a small molecule BCR-abl kinase inhibitor for the treatment of chronic myelogenous leukemia (CML); Tarceva®, a small molecule inhibitor of the EGFR pathway kinase activity for the treatment of non-small cell lung carcinomas, and Nexavar®, a small molecule multi-kinase inhibitor  (CRAF, BRAF, mutant BRAF, Kit, VEGFR-2, VEGR-3, FLT-3) for the treatment of advanced kidney cancer; Sutent®, a small molecule multi-kinase inhibitor for the treatment of gastrointestinal stromal tumors and advanced kidney carcinoma; Sprycel®, a small molecule dual inhibitor of Abl/Src kinases for the treatment of acute lymphoblastic leukemia (ALL) and CML; and Tykerb®, a small molecule dual HER1/HER2 receptor kinase inhibitor for refractory breast cancer. 

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.