NCI Drug Dictionary definition:
An orally bioavailable small molecule with potential antineoplastic activity. Selumetinib inhibits mitogen-activated protein kinase kinases (MEK or MAPK/ERK kinases) 1 and 2, which may prevent the activation of MEK1/2-dependent effector proteins and transcription factors, and so may inhibit cellular proliferation in MEK-overexpressing tumor cells. MEK 1 and 2 are dual-specificity kinases that are essential mediators in the activation of the RAS/RAF/MEK/ERK pathway, are often upregulated in various tumor cell types, and are drivers of diverse cellular activities, including cellular proliferation.
Publications describing human trial results:
Tanios Bekaii-Saab, Mitch A. Phelps, Xiaobai Li, Motoyasu Saji, Laura Goff, John Sae Wook Kauh, Bert H. O'Neil, Stephanie Balsom, Catherine Balint, Ryan Liersemann, Vasily V. Vasko, Mark Bloomston, William Marsh, L. Austin Doyle, Gilian Ellison, Michael Grever, Matthew D. Ringel, Miguel A. Villalona-Calero.
Multi-Institutional Phase II Study of Selumetinib in Patients With Metastatic Biliary Cancers.
Journal of Clinical Oncology, 2011; DOI: 10.1200/JCO.2010.33.9473
Bert H. O'Neil, Laura W. Goff, John Sae Wook Kauh, Jonathan R. Strosberg, Tanios S. Bekaii-Saab, Ruey-Min Lee, Aslamuzzaman Kazi, Dominic T. Moore, Maria Learoyd, Richard M. Lush, Said M. Sebti, and Daniel M. Sullivan.
Phase II Study of the Mitogen-Activated Protein Kinase 1/2 Inhibitor Selumetinib in Patients With Advanced Hepatocellular Carcinoma.
Journal of Clinical Oncology, 2011; DOI: 10.1200/JCO.2010.33.9432
Current Trials Potentially Relevant for GIST Patients