Abstract
Background: Mitotic kinesins are attractive targets in cancer chemotherapy. A large number of small-molecule inhibitors of kinesin spindle protein (KSP) and centromere-associated protein E (CENP-E) have been discovered. Objective: To estimate the therapeutic potential of mitotic kinesin inhibitors. Methods: We comprehensively summarized and analysed the trend among recent patents and conducted a literature review of clinical trials performed since July 2004. Results/conclusion: More than 80 patent applications have been made, spanning a wide range of structural diversity. Five KSP inhibitors and one CENP-E inhibitor have advanced to the early clinical stage, and some of the results for these clinical trials have been disclosed. The therapeutic potential for mitotic kinesin inhibitors is likely to become obvious within the next few years.