Research & Development

CYC116 Aurora Kinase & VEGFR2 Inhibitor

Aurora kinases are a family of serine/threonine protein kinases that are only expressed in actively dividing cells and are crucial for the process of cell division or mitosis. These kinases are often found to be over expressed in many solid tumors, including breast, colon, pancreatic and bladder tumors. Recent genetic evidence suggests that the human Aurora A kinase gene is linked to cancer susceptibility. Aurora B is over expressed in a wide range of tumors, and it has also been shown that its inhibition leads to "catastrophic" (failed) mitosis and rapid cell death. Aurora kinases A & B were discovered by Cyclacel Pharmaceuticals' Professor David Glover.

As important regulators of both genomic integrity and cell cycle progression in cancer cells, the Aurora kinases represent an attractive target for anticancer drug development. Cyclacel Pharmaceuticals has identified a series of compounds acting through inhibition of Aurora kinases which are being developed for oncology therapeutic applications. Several compounds have demonstrated efficacy by oral administration in hematological and solid tumor models with a mechanism consistent with inhibition of the target.

The lead compound in the Aurora kinase inhibitor program, CYC116, is an orally-active inhibitor of Aurora kinases A & B and VEGFR2. CYC116 has been evaluated in a Phase I study in patients with advanced solid tumors.