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Preclinical data on new Angiochem oncology programs published in Journal of Medicinal Chemistry


Targeting of LRP-1 Receptor Increases
Chemotherapeutic Potential for Cancers

Montreal, Canada – Angiochem, Inc. a clinical-stage biotechnology company developing drugs that are uniquely capable of crossing the blood-brain barrier through LRP-1 targeting, published preclinical data on its new oncology programs in the Journal of Medicinal Chemistry.  In the article entitled, “New Angiopep-Modified Doxorubicin (ANG1007) and Etoposide (ANG1009) Chemotherapeutics With Increased Brain Penetration", Che,, 11.10.09, published online March 8, 2010, Angiochem researchers demonstrated that these two  new compounds, derived through the Angiochem EPiC platform, effectively crossed the blood-brain-barrier (BBB) and achieved efficient penetration rates in the brain and in cancer tumor tissue, compared to traditional chemotherapeutics alone.

“Traditionally, chemotherapeutics have had limited efficacy in treating malignant brain tumors due to their inability to permeate the blood brain barrier. In contrast, Angiochem’s EPiC platform exploits the endogenous LRP-1 receptor-mediated transcytosis to  effectively crosses the BBB and achieved therapeutic concentrations of chemotherapeutics in the brain,” said Jean-Paul Castaigne, MD, President and CEO of Angiochem. “These data generated on our earlier-stage compounds builds upon the growing body of clinical evidence we are establishing with ANG1005, our phase 2 product candidate in development for brain cancers, that is embarking on the pivotal stage of development.”

In this article, the role of the EPiC platform to transport across brain capillary endothelial cells via LRP-1 mediated mechanism is described and validated. Angiochem researchers evaluated the potential of twoNCE , ANG1007 and ANG1009 (derivative of doxorubicin and etoposide), to penetrate the brain to treat brain tunors in comparison to traditional chemotherapeutics alone.  . Both agents killed cancer cell lines in vitro with similar cytotoxic activity as unconjugated chemotherapeutics, and exhibited dramatically higher BBB penetration rates and pooled within brain and tumor tissue.

About AngioChem // Angiochem is a clinical-stage biotechnology company discovering and developing new breakthrough drugs that are uniquely capable of crossing the blood-brain barrier (BBB) to treat brain diseases. The company’s proprietary Engineered Peptide Compounds (EPiC) technology creates drugs that cross the BBB and reach therapeutic concentration in the brain, by harnessing naturally-occurring receptors on the surface of the BBB. Angiochem’s lead product candidate, ANG1005 is in two separate clinical studies in patients with brain cancers and cancer metastases. Additionally, Angiochem is developing a deep and broad product pipeline, including small and large molecules, for the potential treatment of a wide range of CNS diseases, including neurodegenerative and metabolic diseases, brain cancer, psychiatric disorders and many others. Founded in 2006, Angiochem maintains headquarters in Montreal, Canada. For additional information about the Company, please visit: