WX-554

The oral small-molecule MEK inhibitor (WX-554) was acquired from UCB at the beginning of 2009 and is progressing towards clinical development under WX-554.

The mitogen-activated protein kinase (MEK) has been shown to play a central role in signal transduction. MEK has been linked to a multitude of biological processes such as cell division, cell differentiation and cell death. The MEK signalling pathway is overexpressed in more than 30 % of cancers, resulting in uncontrolled cell growth and proliferation. Inhibition of MEK could have significant therapeutic potential.

Status

The first dose in man has been administered in November 2009. The open-label dose escalation study in healthy male volunteers investigates pharmacokinetics, pharmacodynamics as well as safety and tolerability of WX-554. The trial aims to determine the optimal biological dose for the inhibition of the MEK-system by WX-554.