Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Cancer

MEK

Cell culture and mouse studies suggest the MEK inhibitor Mekinist trametinib could be useful for treating K-Ras (KRAS)-mutant cancers. In a mouse model of Kras-mutant pancreatic cancer, Craf (Raf1)-targeting shRNAs promoted MEK inhibitor-induced growth suppression, suggesting resistance to MEK inhibitors in such cancers could be driven by RAF1 signaling. In KRAS-mutant human cancer cells, trametinib, which disrupted the interaction between RAF1 and MEK, decreased proliferation compared with a MEK inhibitor, which did not disrupt the interaction. Next steps could include designing clinical trials to test trametinib and other newer MEK inhibitors in patients with KRAS-mutant cancers.
Japan Tobacco Inc. markets Mekinist to treat melanoma. The drug is also in Phase II testing to treat non-small cell lung cancer (NSCLC) and pancreatic cancer.

SciBX 7(19); doi:10.1038/scibx.2014.554
Published online May 15, 2014

Patent and licensing status unavailable

Lito, P. et al. Cancer Cell; published online April 15, 2014;
doi:10.1016/j.ccr.2014.03.011
Contact: Neal Rosen, Memorial Sloan Kettering Cancer Center, New York, N.Y.
e-mail:

rosenn@mskcc.org
Contact: Scott Lowe, same affiliation as above
e-mail:

lowes@mskcc.org