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Prolexys Pharmaceuticals Initiates Phase 1 Study
Date:8/29/2007

s (cancer genes), including activated RasV12 (Cancer Cell 3, 285-96, 2003). Extensive medicinal chemistry efforts at Prolexys resulted in the discovery of PRLX 93936, a small molecule that is approximately 100 times more potent and 1000 times more soluble than erastin. Application of the company's proprietary chemiproteomics discovery platform identified the mitochondrial outer membrane protein VDAC (Voltage Dependent Anion Channel) as a potential target of erastin (Nature 447: 864-868, 2007), and PRLX 93936.

PRLX 93936 was tested against a series of normal and tumor cell lines derived from tumors with dissimilar causative mutations, indicating potent and selective activity against a wide variety of tumors, many with activated Ras pathway. The compound showed robust tumor regression in a range of human tumor xenografts grown in immuno-compromised mice, including models of pancreatic (PANC-1), colon (DLD1), and ovarian (OVCAR5) cancers, and melanoma (SK-Mel-28), fibrosarcoma (HT-1080) and other solid tumors. PRLX 93936 produced efficacy ranging from tumor-growth inhibition to complete regression in a dose-dependent fashion.

About Prolexys

Prolexys Pharmaceuticals, Inc. is a privately held biopharmaceutical enterprise that discovers small molecules acting on novel targets. Its therapeutic focus is cancer. The Company's ability to identify and validate novel targets is driven by its technological leadership in the field of proteomics and the application of proteomics to drug discovery programs. For more information about Prolexys, please visit http://www.prolexys.com.


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