Locus Pharmaceuticals Announces Research Agreement with Eli Lilly and Company

Locus Pharmaceuticals, Inc., a computationally-based drug design and development company, announced that it has entered into a research agreement with Eli Lilly and Company (NYSE: LLY), whereby Locus will apply its proprietary computational technologies to design small molecule compounds having activity against a protein kinase target identified by Lilly. Financial and other terms of the agreement were not disclosed.

"We are very pleased to be working with Lilly, which we view as a major additional validation of our 'virtual' fragment design approach and our expanding core competence in kinases,' said Jeffrey S. Wiseman, Ph.D., Vice President, Technology & Informatics at Locus. 'Having successfully applied our computational approach to internal kinase programs which have reached the IND lead stage, we are confident that our proprietary algorithms will allow us to design novel chemical classes of kinase inhibitors with predictably high potency and selectivity for Lilly.'

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.

Locus' core technology is fragment-based, computational drug design which Locus has combined with highly integrated medicinal chemistry and biology capabilities.

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 and computes the binding affinity of molecular fragments to these sites. The fragments are then assembled computationally into drug candidates with accurately predicted binding potency. Other Locus technologies model physically realistic, long-range timescales of protein motion and design in appropriate ADMET properties. The result is a 'virtual library' of drug candidates that exceeds the size and diversity of any physical screening library by orders of magnitude. 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, orally-active lead molecules.

About Locus Pharmaceuticals
Locus Pharmaceuticals, Inc. is a world leader in computational drug design. These proprietary computational approaches are combined with in-house expertise in chemistry, biology and crystallography to create a fully integrated drug discovery and development platform.

Locus is developing oral drug therapies to address major unmet medical needs, principally in cancer and inflammation. Locus expects to file an IND early this year for LP-261, Locus' lead oncology compound. In its inflammation program, Locus created uniquely selective p38 inhibitors that target an allosteric binding site rather than the ATP site, which may offer an improved safety profile compared to other p38 compounds under development. Earlier stage projects include a program to develop multi-kinase inhibitors, a Heat Shock Protein 90 program which is being conducted in a collaboration with the National Cancer Institute (NCI) and a gp41 program for AIDS/HIV. All of the Company's development programs emanate from its computational technology. Locus is privately-held. Visit www.locuspharma.com for more information.