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Locus Pharmaceuticals Initiates Clinical Development of Novel Anticancer Drug

Posted on: Thursday, 13 July 2006, 15:00 CDT

Clinical Study of an Orally Administered Small Molecule Compound Cleared by the U.S. Food and Drug Administration; Drug Candidate May Be Useful for the Treatment of Drug Resistant Tumors

Locus Pharmaceuticals, Inc., a computationally based drug design and development company, announced today that it has cleared the 30-day review period by the U.S. Food and Drug Administration (FDA) for its Investigational New Drug (IND) application for LP-261, an orally administered small molecule for the treatment of cancer. A Phase I clinical study will begin shortly.

LP-261, which is predicted to bind to tubulin in a novel way, was developed by Locus using its proprietary computational drug design capabilities. This drug candidate is distinguished by its anti-tumor and anti-angiogenesis combination mechanism, 100% oral bioavailability and potential to treat resistant tumors. The protocol for the Phase I is now before Institutional Review Boards (IRB's) at the sites selected for the trial and clinical supplies are being prepared. The Phase I will be an open-label, dose-escalation study to evaluate the safety and pharmacology of the drug in patients with advanced tumors.

LP-261 acts on tubulin at the colchicine site to induce G2/M arrest and block cell division, the mechanism by which cancer cells proliferate. Tubulin targeting agents make up one of the largest markets in the pharmaceutical industry. There are three recognized binding sites for pharmacologic agents on tubulin: the taxane, vinca and colchicine sites. All of the approved tubulin drugs target either the taxane or vinca sites and are parenterally administered. As a result, LP-261, being orally administered and with a novel colchicine binding mode, would offer a new approach to this well validated target.

In preclinical studies, LP-261 demonstrated broad anti-tumor activity in vitro and, after oral administration, in vivo, including tumor regression in xenograft models of several major solid tumor types. In addition, the compound has demonstrated anti-angiogenic effects in certain angiogenesis models. Importantly, LP-261 has also been shown to be effective in taxol-resistant cells, vinca-resistant cells, and primary leukemia cells isolated from Gleevec-resistant patients. LP-261 does not appear to be a substrate for MDR pumps.

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 highly competitive drug design and 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 Amgen, Dow AgroSciences, Eli Lilly and Ono Pharmaceuticals. 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.

In addition to the LP-261 program, Locus has created uniquely selective p38 inhibitors for its lead inflammation program that target an allosteric binding site rather than the ATP site. This may offer an improved safety profile compared to other p38 compounds under development. Other projects include a program to develop multi-kinase inhibitors, a Heat Shock Protein 90 program which is being conducted in collaboration with the National Cancer Institute (NCI) and a gp41 program for AIDS/HIV. Locus is privately-held. Visit www.locuspharma.com for more information.

Source: Business Wire

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