Description GDC-0973, a selective inhibitor of MEK, also known as mitogen activated protein kinase kinase (MAPKK), is a key component of the RAS/RAF/MEK/ERK pathway, which is frequently activated in human tumors. Inappropriate activation of the MEK/ERK pathway promotes cell growth in the absence of exogenous growth factors.
Development Status A Phase I clinical trial evaluating GDC-0973 for solid tumors, a Phase Ib clinical trial in combination with GDC-0941, a PI3 Kinase Inhibitor, for solid tumors and a Phase Ib clinical trial in combination with vemurafenib, a BRAF inhibitor, for metastatic melanoma are ongoing.
GDC-0973 is being developed in collaboration with Exelixis, Inc. and vemurafenib is being co-developed under a 2006 license and collaboration agreement between Roche/Genentech and Plexxikon, a member of the Daiichi Sankyo Group.
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National Institutes of Health Website: www.clinicaltrials.gov
August 2011