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Nereus Pharmaceuticals Initiates Phase I Clinical Trial for Anti-Cancer Compound NPI-2358

Posted on: Wednesday, 7 June 2006, 09:00 CDT

Nereus Pharmaceuticals, Inc., a pioneer in drug discovery and development from marine microbial sources, has initiated a Phase I clinical trial to evaluate the safety and tolerability of NPI-2358, a novel, small molecule tumor vascular disrupting agent (VDA) for the treatment of patients with solid tumors.

The open label, single-agent study opened to enrollment for patients with advanced solid tumor malignancies at two centers with well known expertise in developing new oncology drugs: the Barbara Ann Karmanos Cancer Institute in Detroit, Michigan, and the CTRC Institute for Drug Development in San Antonio, Texas. Trial participants receive once-weekly, intravenous doses of NPI-2358, which will be escalated to determine maximum tolerated dose. Other objectives include tumor response, pharmacokinetic and pharmacodynamic analyses. The trial is expected to enroll approximately 35 patients.

"We are excited to have treated the first patient, and look forward to applying our experience with Phase I clinical trials and VDAs to a thorough investigation of Nereus' promising new compound," said Dr. Patricia M. LoRusso, principal investigator and Director of the Phase I Clinical Trials Program at the Barbara Ann Karmanos Cancer Institute and Professor of Hematology and Oncology at Wayne State University.

In preclinical models of cancer, including breast, sarcoma, colon and prostate, NPI-2358 demonstrated it is a potent and selective tumor vascular disrupting agent (VDA). NPI-2358 exhibits its effects by interacting at the colchicine-binding site on microtubules. This provokes a rapid collapse and occlusion of established vasculature in the tumor, which induces tumor cell death, leading to necrosis. In in vitro studies, this selective vascular collapse commences within minutes of exposure to the VDA and appears to be caused by the effects of the compound on the shape, cohesiveness and growth of proliferating immature endothelial cells present in the tumor vasculature, but not the dormant and mature endothelial cells in non-tumor vasculature. NPI-2358 also synergizes with chemotherapeutics in human tumor xenograft models. Nereus synthesized NPI-2358 and several other analogues from the parent molecule called Halimide, which originated from a marine fungus.

"Preclinical studies involving various solid tumors demonstrate NPI-2358 selectively destroys vasculature in the central portion of tumors, shrinking the malignant mass," explained Dr. Anthony Tolcher, principal investigator and Director of Clinical Research at the CTRC Institute for Drug Development. "I look forward to continuing to investigate this new generation of VDAs in this clinical trial."

"This is our second novel compound derived from our discovery effort to enter clinical trials, and we're pleased to collaborate with several prestigious research institutions to advance our oncology drug candidates," said Kobi M. Sethna, President and CEO of Nereus Pharmaceuticals, Inc.

About Nereus Pharmaceuticals, Inc.

Nereus Pharmaceuticals pursues untapped sources of chemical diversity to discover and develop novel therapeutics. With unmatched expertise in marine microbiology and integrated technologies to identify and synthesize novel biologically active compounds, the Company's two oncology drug candidates are in Phase I clinical trials. NPI-2358, a tumor vascular disrupting agent, is being evaluated for solid tumors, and proteasome inhibitor NPI-0052 is being developed for solid tumors, lymphomas and multiple myeloma. Nereus' discovery portfolio also includes additional drug candidates for oncology, as well as infectious diseases and inflammation. The Company is privately held and based in San Diego, California. For more information, visit www.nereuspharm.com.

Nereus Pharmaceuticals is a registered trademark of Nereus Pharmaceuticals, Inc.

Source: Business Wire

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