TELK » Topics » TLK60404-Aurora Kinase/VEGFR2 Inhibitors

This excerpt taken from the TELK 10-Q filed May 7, 2009.

TLK60404—Aurora Kinase/VEGFR2 Inhibitors

We currently have a small molecule compound inhibiting both Aurora kinase and VEGFR2 kinase in pre-clinical development. Aurora kinase is a signaling enzyme whose function is required for cancer cell division, while vascular endothelial growth factor receptor, or VEGFR, plays a key role in tumor blood vessel formation, ensuring an adequate supply of nutrients to support tumor growth. The lead compounds of our first dual inhibitor program met a development milestone in August 2008 by demonstrating anticancer activity in preclinical models of human colon cancer and human leukemia. A development drug product candidate, TLK60404, has been selected. We are conducting the required preclinical safety studies that if successful may support the potential filing of an IND application with the FDA.

These excerpts taken from the TELK 10-K filed Mar 2, 2009.

TLK60404—Aurora Kinase/VEGFR2 Inhibitors

We have a small molecule compound inhibiting both Aurora kinase and VEGFR2 kinase. Aurora kinase is a signaling enzyme whose function is required for cancer cell division, while vascular endothelial growth factor receptor, or VEGFR, plays a key role in tumor blood vessel formation, ensuring an adequate supply of nutrients to support tumor growth. The lead compounds of our first dual inhibitor program met a development milestone in August 2008 by demonstrating anticancer activity in preclinical models of human colon cancer and human leukemia. These lead compounds prevented tumor growth in preclinical models of human colon cancer and human leukemia by inhibiting both Aurora kinase and VEGFR2. Our data support the concept that dual inhibition of Aurora kinase and VEGFR2 represents a promising approach for anti-cancer therapy. A development drug product candidate, TLK60404, has been selected. We are conducting the required preclinical safety studies that if successful may support the potential filing of an IND application with the FDA.

TLK60404—Aurora Kinase/VEGFR2 Inhibitors

STYLE="margin-top:6px;margin-bottom:0px; text-indent:4%">We have a small molecule compound inhibiting both Aurora kinase and VEGFR2 kinase. Aurora kinase is a signaling enzyme whose function is required for
cancer cell division, while vascular endothelial growth factor receptor, or VEGFR, plays a key role in tumor blood vessel formation, ensuring an adequate supply of nutrients to support tumor growth. The lead compounds of our first dual inhibitor
program met a development milestone in August 2008 by demonstrating anticancer activity in preclinical models of human colon cancer and human leukemia. These lead compounds prevented tumor growth in preclinical models of human colon cancer and human
leukemia by inhibiting both Aurora kinase and VEGFR2. Our data support the concept that dual inhibition of Aurora kinase and VEGFR2 represents a promising approach for anti-cancer therapy. A development drug product candidate, TLK60404, has been
selected. We are conducting the required preclinical safety studies that if successful may support the potential filing of an IND application with the FDA.

FACE="Times New Roman" SIZE="2">MCP-1 Antagonists (C243)—Small Molecules for Autoimmune and Inflammatory Disorders

Inflammation
is an important response of the body to injury and infection. If inflammation becomes excessive or prolonged, it can lead to pathological conditions, including asthma, inflammatory bowel disease, multiple sclerosis, psoriasis, rheumatoid arthritis
and septic shock. An early step in the inflammatory response is the attraction of white blood cells, or leukocytes, from the circulatory system to damaged or infected tissue by messenger molecules called chemokines.

STYLE="margin-top:12px;margin-bottom:0px; text-indent:4%">Using our TRAP technology we discovered MCP-1 antagonists, including our lead compound C243, a small molecule that prevents leukocyte infiltration, a
process linked to tissue injury in chronic autoimmune and inflammatory diseases such as multiple sclerosis, rheumatoid arthritis and atherosclerosis. In February 2007, we announced an agreement with SRI International under which SRI will fund and
conduct preclinical studies of C243 in multiple sclerosis and other autoimmune and inflammatory diseases. We hold exclusive commercialization rights to the MCP-1 antagonists, including C243, in North and South America. Our former collaborator,
Sanwa, holds exclusive rights in Asia, and we have non-exclusive rights in the rest of the world.

TLK60404—Aurora Kinase/VEGFR2 Inhibitors

We currently have a small molecule compound inhibiting both Aurora kinase and VEGFR2 kinase in pre-clinical development. Aurora kinase is a signaling enzyme whose function is required for cancer cell division, while vascular endothelial growth factor receptor, or VEGFR, plays a key role in tumor blood vessel formation, ensuring an adequate supply of nutrients to support tumor growth. The lead compounds of our first

 

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dual inhibitor program met a development milestone in August 2008 by demonstrating anticancer activity in preclinical models of human colon cancer and human leukemia. A development drug product candidate, TLK60404, has been selected. We are conducting the required preclinical safety studies that if successful may support the potential filing of an IND application with the FDA.

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