MET Kinase Inhibitor for Solid Tumors

SGX523, an internally developed, orally-bioavailable, small molecule inhibitor of the MET receptor tyrosine kinase is currently in Phase I clinical studies (www.clinicaltrials.gov). SGX523 has shown significant selectivity for the MET receptor tyrosine kinase over more than 200 protein kinases and has demonstrated both potent in vitro blockade of the activity of this cancer target and in vivo activity against human cancer cells that depend on MET for their uncontrolled growth and proliferation.

 Publicly available data indicates that the MET receptor tyrosine kinase plays important roles in controlling cell growth, division and motility, metastasis, and the formation of blood vessels, and is implicated as a causative agent in a broad range of solid tumors, including lung, colon, prostate, gastric, and both hereditary and acquired forms of certain kidney cancers.