Xl184
 

http://www.exelixis.com/pipeline/xl184

XL184 is a small molecule designed to inhibit multiple receptor tyrosine kinases, specifically MET and VEGFR2. MET is a receptor tyrosine kinase that plays key roles in cellular proliferation, migration, and invasion as well as angiogenesis<SUP>1</SUP>. These biological processes contribute to the transformation, progression, survival and metastasis of cancer cells<SUP>1</SUP>. The MET pathway is frequently activated in tumors through MET amplification, mutation, and overexpression, as well as through overexpression of its ligand HGF<SUP>1</SUP>. Expression of VEGF has been observed in a variety of cancers and has been associated with the stimulation and growth of new blood vessels to support the tumor<SUP>2,3</SUP>. MET and VEGFR2 are important driving forces in angiogenesis, implicated in the ability of tumors to overcome hypoxia following angiogenesis inhibition<SUP>4,5</SUP>.

1. Christensen JG, Burrows J, Salgia R. c-Met as a target for human cancer and characterization of inhibitors for therapeutic intervention. Cancer Lett. 2005; 225(1):1-26.
2. Sandler A. Bevacizumab in non-small cell lung cancer. Clin Cancer Res. 2007; 13 (15 Suppl): 4613s-4616s.
3. Heath VL and Bicknell R. Anticancer strategies involving the vasculature. Nat Rev Clin Oncol. 2009; Jul;6(7):395-404.
4. You WK and McDonald DM. The hepatocyte growth factor/c-Met signaling pathway as a therapeutic target to inhibit angiogenesis. BMB Reports. 2008; 41:833–839.
5. Schmidt C. Why do tumors become resistant to antiangiogenesis drugs? J. Natl. Cancer. Inst. 2009;101:1530–1532.

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Solid tumor STUDY
http://www.clinicaltrials.gov/ct2/sh...ow_locs=Y#locn


Exelixis Shares Soar on Cancer Results

Luke Timmerman 11/18/10

LINK

Exelixis (NASDAQ: EXEL), the South San Francisco-based developer of cancer drugs, saw its shares climb 32 percent to $6.23 today after reporting on clinical trial results for its lead product candidate against prostate cancer. The company reported that 19 out of 20 patients who got its experimental XL184 treatment had at least partial clearance of lesions on their bones where the cancer had spread. The findings were released at the EORTC-NCI-AACR meeting in Berlin, Germany. Xconomy reported on what this clinical trial data means to Exelixis in an in-depth feature story last month.