Prolexys Pharmaceuticals Initiates Phase 1 Study

Main Category: Cancer / Oncology
Also Included In: Clinical Trials / Drug Trials
Article Date: 30 Aug 2007 - 0:00 PDT

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Prolexys Pharmaceuticals, Inc. announced that its first-in-humans Phase 1 study of PRLX 93936 has begun. This open-label trial is designed to evaluate the safety, pharmacokinetic and pharmacodynamic properties of PRLX 93936 in patients with advanced solid tumors. Study sites include TGen Clinical Research at Scottsdale Healthcare in Scottsdale, Arizona, and Tower Cancer Research Foundation in Beverly Hills, California. The first Phase 1 study will be a dose-escalating trial involving up to 36 patients.

"We are enthusiastic about our participation in the study of this interesting new agent with what appears to be a unique mechanism of action," said Dr. Daniel Von Hoff, Physician-in-Chief and Director of Clinical Research at TGen, and the principal investigator for the study at Scottsdale Healthcare. "Rarely have we seen pre-clinical anti-tumor effects that match those produced by PRLX 93936. We're very hopeful that this compound will have a therapeutic effect in patients with tumors that are non-responsive to existing therapeutic agents."

"The initiation of this Phase I clinical trial demonstrates our commitment to develop novel approaches to cancer therapies based on the company's proteomics technology platform," said David Clark, President and CEO of Prolexys.

"Based on the broad anti-cancer activity we have seen in pre-clinical models, we are looking forward to evaluating the potential anti-cancer activity in humans for this new drug candidate," stated Dr. Sudhir Sahasrabudhe, Prolexys' Chief Scientific Officer.

About PRLX 93936

PRLX 93936 is a structural analog of a compound called erastin, in-licensed by Prolexys from the MIT/ Whitehead Institute in January 2005. Erastin was identified as a potential anti-cancer therapeutic in a screen against cell lines engineered to differentially express several oncogenes (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.

Prolexys Pharmaceuticals, Inc.
http://www.prolexys.com