Telik Reports Preclinical Results at AACR Annu...( Anti-Tumor Efficacy and Molecula...)

Anti-Tumor Efficacy and Molecular Mechanism of TLK58747; Abstract # 4515

Telik researchers identified a novel alkylating agent, TLK58747, which functions as a prodrug, without the need for enzymatic processing, and which does not release an activation byproduct known to be associated with toxicity of other alkylating agents (acrolein).

Key findings:

• TLK58747 inhibited the growth of nine established cell lines of various tumor types and retained its effectiveness against cancer cell lines resistant to standard cancer chemotherapeutics including adriamycin, paclitaxel, and carboplatin.
• Treatment of human cancer cells with TLK58747 led to the activation of the DNA damage-response pathway, and produced G2/M cell cycle arrest in human solid tumor cell lines. The resulting apoptosis or senescence of these cells may depend on their p53 status.
• In vivo, TLK58747 demonstrated significant antitumor activity both orally and parenterally against a wide variety of human tumor types, including breast, pancreatic, prostate, and colorectal carcinomas, as well as glioma and promyelocytic leukemia.

Telik, Inc. of Palo Alto, CA, is a clinical stage drug development company focused on discovering and developing small molecule drugs to treat cancer and inflammatory diseases. The company's most advanced investigational drug candidates in clinical development are TELINTRA(R), a modified glutathione analog for the treatment of cytopenias due to myelodysplastic syndrome or chemotherapy, and TELCYTA(R), a tumor-activated prodrug for the treatment of advanced ovarian cancer and non-small cell lung cancer. Telik's product candidates were discovered using its proprietary drug discovery technology, TRAP(R), which enables the rapid and efficient discovery of small molecule drug candidates.

TELIK, the Telik logo, TELI
'/>"/>