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Telik Reports Preclinical Results at AACR Annual Meeting
Date:4/28/2009

PALO ALTO, Calif., April 28 /PRNewswire-FirstCall/ -- Telik, Inc. (Nasdaq: TELK) announced results of studies on two of its drug development programs that were presented at the 100th annual meeting of the American Association for Cancer Research (AACR) in Denver, CO. The abstracts can be found on the Telik website, www.telik.com.

In vivo Characterization and Mechanism of Action of Orally Active Aurora Kinase/ VEGFR Inhibitors; Abstract # 1764

Aurora kinases are Ser/Thr kinases that play an important role in chromosome alignment, segregation and cytokinesis during mitosis. Over-expression of Aurora kinases has been demonstrated in both solid tumors and leukemia and is considered to be associated with aneuploidy and carcinogenesis. Inhibition of Aurora kinase activity induces growth arrest and apoptosis in cells and leads to tumor-growth inhibition in xenograft models of human cancer.

Key findings:

  • Telik researchers presented additional data for a novel class of small molecule drug candidates showing strong and equipotent inhibition of Aurora kinase and VEGFR kinase, with IC50s less than 10 nM.
  • These compounds induced growth arrest, polyploidy and apoptosis in human cancer cell lines, such as HCT116 (colon), HL60 (promyelocytic leukemia) and A549 (lung) - reflecting cell lines with intact or defective p53-dependent post-mitotic checkpoints.
  • More than 80% inhibition of tumor growth was seen in an HL60 xenograft model following a once daily oral dosing schedule.
  • Drug inhibition of aurora kinase and VEGFR activity in tumor samples of treated animals was established by analysis of markers, such as histone H3 phosphorylation and CD31.


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