WX-554
ENGLISH DEUTSCH
| Compound Class | Orally available small molecule MEK inhibitor |
| Indication | Various cancers |
| Target | mitogen-activated protein kinase (MEK) |
| Mode of Action | 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 differentation and cell death. The MEK signalling pathway is overexpressend in more than 30 % of cancers, resulting in uncontrolled cell growth and proliferation. Inhibition of MEK could have significant therapeutic potential. |
| Development Status | In June 2010 WILEX published final results of the dose escalation study. In addition to safety and tolerance, the pharmacokinetic and pharmacodynamic properties of the MEK inhibitor were also investigated. The substance was safe and well tolerated in the 25 healthy volunteers. The MEK signal transduction pathway was inhibited in a dose-dependent matter reaching complete inhibition at 1 mg/kg body weight. The study, which was conducted in Germany, tested five increasing dose levels, each administered once by a 15 min infusion of WX554 in five healthy male volunteers.In January 2012 WILEX successfully completed a Phase I dose escalation study with the oral MEK inhibitor WX-554 in healthy volunteers. WX-554 showed very good bioavailability and inhibition of the MEK signal transduction pathway in a dose-dependent manner achieving long-lasting inhibition at 100 mg. A Phase Ib/II study in cancer patients was started in April 2012. |
| History | WILEX acquired an MEK inhibitor from UCB Pharma S.A., Brussels, Belgium, as a preclinical project and started clinical development under the code WX-554. |
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