MK-5108 (VX-689) is an Aurora kinase inhibitor being developed in collaboration with Merck for the treatment of cancer. Aurora kinases are key enzymes involved in the cell cycle and are implicated in the growth and proliferation of tumor cells in a variety of solid tumor cancers. As enzymes specific for and essential to cell growth and division, Aurora kinases hold the potential to be important control points for slowing the growth and spread of tumors. Aurora kinases are known to be overexpressed in a number of tumor types, including colon cancer, breast cancer, ovarian cancer and other cancers as well as in lymphoma and leukemia.
In mid-2008, Merck initiated a Phase 1 clinical trial of the Aurora kinase inhibitor MK-5108 (VX-689) in patients with advanced and/or refractory solid tumors. Merck has discontinued development of MK-0457 (VX-680), another Aurora kinase inhibitor that it had been developing under the collaboration.
Aurora kinase research and related compounds
The Aurora kinase inhibitors being evaluated in collaboration with Merck were discovered by scientists at Vertex's Oxford, U.K. research site as part of a broad research effort targeting the kinase gene family. Vertex researchers published the three-dimensional atomic crystal structure of Aurora-A kinase in 2002, a key scientific advance that enabled the design and optimization of multiple classes of small molecule Aurora kinase inhibitors.