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Paloma Pharmaceuticals Presents at the AACR-NCI-EORTC International Conference Molecular Targets and Cancer Therapeutics
Date:11/16/2009

JAMAICA PLAIN, Mass., Nov. 16 /PRNewswire/ -- Paloma Pharmaceuticals, Inc. announced it will give a presentation today at the AACR-NCI-EORTC International Conference Molecular Targets and Cancer Therapeutics, "Palomid 529, a dual mTor1/2 inhibitor, efficiently penetrates the blood brain barrier and may be an attractive agent for treatment of glioblastoma" by Dr. Olaf van Tellingen, Ph.D. of The Netherlands Cancer Institute, Amsterdam, The Netherlands.

(Logo: http://www.newscom.com/cgi-bin/prnh/20081117/NEM057LOGO )

Palomid 529 (P529) is a non-steroidal, synthetic, small molecule anti-tumor agent created through computational design, synthetic and medicinal chemistry, the result of three generations of Palomid design work. Palomid's broad activity as an anti-tumor agent is shown to reside in its ability to target and inhibit the PI3K/Akt/mTOR signal transduction pathway as a dual TORC1/TORC2 inhibitor.

"Glioblastoma Multiforme is the most frequent primary brain tumor for which very few active drugs are available. The blood brain barrier is a major obstacle in the efficient delivery of drugs to the brain. In particular, the activities of ABC transporters such as P-glycoprotein and breast cancer-resistance protein (BCRP) are important. We were, therefore, pleased to see that Palomid 529 is only a very weak substrate of P-glycoprotein and BCRP and that high brain-to-plasma ratios were achieved following drug administration. This property makes Palomid 529 an attractive candidate for targeting this potentially important PI3K-Akt-mTOR signal transduction route in brain cancer," said Dr. Van Tellingen.

"Work form the laboratory of Dr. van Tellingen is significant in that it shows administration of P529 penetrates the brain-blood-barrier, enters the brain and is not affected by the ABC transporters -- a common problem in cancer
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SOURCE Paloma Pharmaceuticals, Inc.
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