LOCUS PHARMACEUTICALS ENTERS INTO SECOND DRUG DISCOVERY AGREEMENT ON KINASES WITH ONO PHARMACEUTICAL CO., LTD.
BLUE BELL, PA - November 5, 2007 - Locus Pharmaceuticals, Inc., a clinical stage computationally-based drug design and development company, announced today that it has entered into a second research agreement with Ono Pharmaceutical Co., Ltd. Based on this agreement, Locus will apply its proprietary computational technologies and capabilities in chemistry, biology and crystallography to design and develop IND-directed preclinical drug candidates for Ono. The molecular target is a protein kinase newly selected by Ono. Financial and other terms of the agreement were not disclosed.
In July, 2006, Ono and Locus entered into a drug discovery agreement targeting a kinase selected by Ono with the goal of identifying small molecule inhibitors of the targeted kinase. Since the start of this collaboration, Locus has successfully applied its proprietary technology and fragment-based virtual libraries to fully characterize the collaboration target, identify potent and patentable inhibitors and is in the process of optimizing novel IND lead candidates.
Based on the progress achieved in the ongoing collaboration and Ono's appreciation of Locus' unique capabilities in its integrated drug discovery approach, Ono decided to start a second collaboration with Locus on a newly selected kinase.
"We are pleased with the progress of our existing Ono collaboration and are strongly encouraged by the confidence expressed by Ono to initiate a second discovery program," said H. Joseph Reiser, Ph.D., President and Chief Executive Officer of Locus. "Having now applied our leading computational technology to many drug discovery targets including kinases, we enter this new collaboration with increased confidence to deliver strong results."
Protein kinases function as control switches for many biochemical pathways inside cells. Kinase activities can become dysregulated by numerous molecular and signaling events, thus contributing to both the onset and progression of diseases. These proteins are of particular interest as targets for the development of novel therapeutics, but because there are more than 500 structurally related kinases, a drug often requires high selectivity for the intended target, a design capability where Locus has demonstrated expertise.
"We highly appreciate the competitive Locus infrastructure for drug discovery which effectively integrates their proprietary computational approaches," said Kazuhito Kawabata, Ph.D., Executive Director of Strategic Alliance Headquarters, Ono. "We are glad to expand our collaboration and look forward to realizing high value drug candidates."
Locus' computational technologies to design small molecule drug candidates
Starting with a protein crystal structure, an in silico collection of 40,000 molecular fragments and one of the world's largest privately-owned Linux-based supercomputer clusters, Locus identifies optimum ligand binding sites on protein targets, computes the binding affinity of molecular fragments to those sites and then links fragments with desirable chemical properties to computationally assemble virtual drug candidates. The result is a ‘virtual library' of drug candidates that exceeds the size and diversity of any physical screening library by orders of magnitude.
In addition, Locus can simulate physically realistic protein motions on very long-range timescales which can be used to validate the biological relevance of novel binding sites that may be uncovered by fragment mapping studies. Because of the speed and accuracy with which these virtual libraries are constructed and evaluated, Locus typically needs to synthesize only hundreds of compounds to generate highly potent lead molecules.
About Locus Pharmaceuticals
Locus Pharmaceuticals, Inc. is a world leader in computational drug design. Locus has effectively integrated its proprietary computational approaches with in-house expertise in chemistry, biology and crystallography to create a competitive preclinical drug development platform.
Locus is using its capabilities to develop its own compounds and has also entered into various drug design/development collaborations with pharmaceutical partners, including Ono. All of the Company's internal development programs emanate from its computational technology and are focused on oral drug therapies, principally in cancer and inflammation. Locus' lead oral oncology compound, LP-261 is in late Phase I studies and is expected to enter Phase II studies in early 2008. In its inflammation program, Locus created uniquely selective, first in class p38 inhibitors that bind to an allosteric binding site rather than the ATP site, which may offer an improved safety profile. Locus expects to file an IND for p38 in 2008. Locus has identified an orally active multi-kinase inhibitor for cancer currently in preclinical development, with an expected IND filing in 2008. Locus is also working on earlier stage projects targeting Heat Shock Protein 90 which is being conducted in collaboration with the National Cancer Institute (NCI), an EPO antagonist program in collaboration with the National Institute of Health (NIH) and an oral gp41 program for AIDS/HIV.
Locus is a privately-held company. Visit www.locuspharma.com for more information.