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Nereus Pharmaceuticals Reports Positive Preclinical Results of Anti-Cancer Drug Candidates Derived from Marine Microbes at AACR Annual Meeting.


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AACR AACR American Association for Cancer Research
AACR Anglo-American Cataloging Rules
AACR Australasian Association of Cancer Registries
AACR African Armed Conflicts Resolved
 Annual Meeting 2004

SAN DIEGO--(BUSINESS WIRE)--March 29, 2004

Nereus Pharmaceuticals Inc., a pioneer in drug discovery and development from marine microbial sources, will report on the progress of its proteasome inhibitor and its vascular targeting agent, both of which demonstrate anti-cancer activities. Nereus will present this data during two poster sessions at the 95th Annual Meeting of the American Association for Cancer Research Wikipedia is not the place for advertisement or self-advertising.

The American Association for Cancer Research (AACR) is an organization based in Philadelphia, Pennsylvania, that focuses on all aspects of cancer research including basic, clinical and translational
, March 27-31, 2004, in Orlando, Florida:

"NPI-2358: A Novel Diketopiperazine, Induces Tubulin tubulin /tu·bu·lin/ (too´bu-lin) the constituent protein of microtubules.

tu·bu·lin
n.
A globular protein that is the structural constituent of microtubules.
 Depolymerization depolymerization /de·po·lym·er·iza·tion/ (de?po-lim?er-i-za´shun) the conversion of a polymer into its component monomers.

depolymerization
 In Vitro and Tumor Vascular Collapse In Vivo"

Nereus plans to submit an Investigational New Drug (IND) application to the U.S. Food and Drug Administration (FDA FDA
abbr.
Food and Drug Administration


FDA,
n.pr See Food and Drug Administration.

FDA,
n.pr the abbreviation for the Food and Drug Administration.
) by year-end to initiate human trials for NPI-2358, its lead product candidate. NPI-2358 is a structurally novel, orally active, vascular targeting agent that was developed from a lead molecule isolated from a marine Aspergillus Aspergillus

Any fungus of the genus Aspergillus of the Fungi Imperfecti (form-class Deuteromycetes). Species for which the sexual phase is known are placed in the order Eurotiales. A. niger causes black mold on some foods; A. niger, A. flavus, and A.
 sp. NPI-2358 binds at or near the colchicine-binding site on tubulin and exerts a marked inhibition of tubulin polymerization, resulting in a shortening of polymer length of purified tubulin and in a disruption of the fine network of (alpha)-tubulin staining in human umbilical vein endothelial cells. The compound exhibits activity against several human tumor cell lines and maintains full activity in multi-drug resistant tumor cell lines. NPI-2358 also synergizes with reference chemotherapeutics in human tumor xenograft models. In addition, intravital intravital /in·tra·vi·tal/ (-vit´'l) occurring during life.

in·tra·vi·tal
adj.
Occurring in or performed on a living organism.



intravital

occurring during life.
 microscopy using a murine pseudo-orthotopic breast cancer model showed that NPI-2358 induces a rapid decrease in tumor blood flow resulting in tumor vascular collapse and central necrosis in established tumors. Saskia T.C. Neuteboom, Ph.D., Nereus' director of oncology research and development, will present this poster on Wednesday, March 31. Details are provided in AACR abstract #5419 and available at www.aacr.org.

"NPI-0052: Development of a Structurally and Biologically Novel, Oral Proteasome Inhibitor"

Preclinical data from Nereus' NPI-0052 program demonstrate the potential use of the compound to treat cancer and inflammation, and Nereus expects to file an IND application with the FDA in 2005. NPI-0052, an orally active, highly potent proteasome inhibitor in preclinical development, was discovered during the fermentation of Salinospora, a new marine Gram-positive actinomycete actinomycete

Any of a group of generally low-oxygen–utilizing bacteria identified by a branching growth pattern that results in large threadlike structures. The filaments may break apart to form rods or spheroidal shapes. Some actinomycetes can form spores.
. An important distinguishing feature of NPI-0052, when compared to other proteasome inhibitors, is its inhibition of the three predominant catalytic activities associated with proteasome Proteasomes are large protein complexes inside all eukaryotes and archaea, as well as in some bacteria. In eukaryotes, they are located in the nucleus and the cytoplasm.[1]  function. Studies at Nereus using various cell-based models have also shown that NPI-0052 inhibits the activation of NF-(kappa)B, an important regulatory factor in both cancer and inflammation. In addition, NPI-0052 induces apoptosis in various multiple myeoloma and prostate tumor cell lines, which are characterized by constitutively active NF-(kappa)B. In vivo studies have shown that NPI-0052 is well tolerated after single or repeated intravenous or oral dosing. Michael A. Palladino, Jr., Ph.D., Nereus' chief technical officer and scientific co-founder, will present this poster (#2050) today, March 29 and the abstract is available at www.aacr.org.

"Nereus is excited that these compounds will be the first from our marine microbial discovery program to enter the clinic," said Kobi M. Sethna, president and CEO (1) (Chief Executive Officer) The highest individual in command of an organization. Typically the president of the company, the CEO reports to the Chairman of the Board.  of Nereus Pharmaceuticals. "We are currently seeking collaborators interested in working with us to accelerate the development of NPI-2358 and NPI-0052."

About Nereus Pharmaceuticals

Nereus Pharmaceuticals is an innovative drug discovery and development company pursuing untapped sources of chemical diversity. With unmatched expertise in marine microbiology and structural elucidation, Nereus is using its integrated platform technologies to identify novel biologically active compounds. The company believes that its marine microbes will be the next great source of drug discovery for the pharmaceutical industry. Nereus aims to develop and optimize drug candidates to treat cancer, infectious diseases and inflammation. The company is privately held and based in San Diego, California “San Diego” redirects here. For other uses, see San Diego (disambiguation).
San Diego is a coastal Southern California city located in the southwestern corner of the continental United States. As of 2006, the city has a population of 1,256,951.
. For more information, visit www.nereuspharm.com.

Nereus Pharmaceuticals is a registered trademark of Nereus Pharmaceuticals, Inc.
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Publication:Business Wire
Geographic Code:1USA
Date:Mar 29, 2004
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