5HT-2A inverse agonist:
SOURCE: Arena Pharmaceuticals, Inc.
Arena Pharmaceuticals, Inc. Announces Grant of First U.S. Patent; Method Claims Directed to CART-Discovered Inverse Agonist Compounds
SAN DIEGO, Aug. 22 /PRNewswire/ -- Arena Pharmaceuticals, Inc. (Nasdaq: ARNA - news) today announced the issuance of United States Patent Number 6,107,324 entitled ``Non-Endogenous Constitutively Activated Human Serotonin Receptors and Small Molecule Modulators Thereof.'' This is the first patent issued to Arena since its inception in April of 1997. The patent claims are directed to methods of modulating, by inverse agonism, the activity of a human serotonin receptor, referred to as the ``5HT2A'' receptor, using small molecule compounds discovered using Arena's CART(TM) Technology.
Inverse agonists are a class of chemical compounds that reduce the functional activity of a receptor drug target. Inverse agonists work differently than traditional receptor antagonists, which block the binding of the receptor's native ligand to the receptor. The 5HT2A receptor has been established to be a drug target for the development of therapeutics useful in the treatment of schizophrenia. However, traditional drug discovery efforts in this area have focused on the development of antagonists that block the native ligand for the 5HT2A receptor from binding to this receptor. Using a different approach, Arena utilized its proprietary CART Technology to directly identify inverse agonists to the receptor, without relying on the use of the receptor's native ligand for this identification process. Two of the compounds are being investigated in animal models of schizophrenia, and based upon preliminary data, Arena believes that these experimental compounds are as effective and better tolerated than antipsychotics presently used clinically.
``We formed Arena to primarily advance our CART Technology with respect to ligand-independent drug discovery at orphan receptors,'' stated Jack Lief, Arena's President & CEO. ``Unlike traditional drug discovery techniques, CART does not require prior identification and use of the receptor's ligand. This same approach can also be applied to receptors for which the native ligand has been identified. By using a CART-activated version of the 5HT2A receptor, and not the natural version of this receptor, we not only discovered a novel class of inverse agonist modulators of the receptor, but we believe that we also established the broad applicability of CART.'' Mr. Lief further noted that, ``These compounds were discovered and subjected to preliminary evaluation over an 18 month period. Arena is continuing with internal evaluation of these compounds, and if these continue to proceed in a positive direction, we intend to out-license these compounds, and the related intellectual property, for human clinical evaluation.'' The patent is co-assigned to Arena and Tripos, Inc. (Nasdaq: TRPS - news), Arena's development partner for this program.
Arena's CART Technology allows for the direct identification of modulators of G protein-coupled receptors (GPCR) in a ligand-independent manner, making the technology particularly useful with respect to the over 2,000 orphan GPCRs that are estimated to be a part of the human genome. Such ligand independent screening is made possible by genetic alteration of these receptors, using routinely applicable and proprietary genetic cassettes. The 5HT2A receptor is a GPCR. Arena has established CART Technology collaborations with Eli Lilly and Company, Fujisawa Pharmaceutical Co., Ltd., Taisho Pharmaceutical Co., Ltd., Lexicon Genetics, Inc. and Neurocrine Biosciences, Inc.
The statements made in this press release contain certain forward-looking statements that involve a number of risks and uncertainties. Actual events or results may differ from Arena's expectations. For example, the timing, success and cost of preclinical research, out-licensing endeavors and clinical studies, the risk factors listed in Arena's SEC filings including but not limited to its Form S-1, may affect the actual results achieved by Arena. These forward-looking statements represent the company's judgment as of the date of this release. The company disclaims, however, any intent or obligation to update these forward-looking statements.
``Arena Pharmaceuticals'' is a registered U.S. trademark of the company. ``Arena'' and ``CART'' are trademarks of the company. Arena's headquarters are located at 6166 Nancy Ridge Drive, San Diego, CA 92121. On the Internet, please refer to the Investor Relation's Center at Arena's website: arenapharm.com for further information.
SOURCE: Arena Pharmaceuticals, Inc. |
