FDAnews
www.fdanews.com/articles/88375-locus-to-begin-clical-trials-of-anticancer-drug

LOCUS TO BEGIN CLICAL TRIALS OF ANTICANCER DRUG

July 14, 2006

Locus Pharmaceuticals announced that it has cleared the 30-day review period for its investigational new drug application for LP-261, an orally administered small molecule for the treatment of cancer. A Phase I clinical study will begin shortly.

This drug candidate is distinguished by its anti-tumor and anti-angiogenesis combination mechanism, 100 percent oral bioavailability and potential to treat resistant tumors. The Phase I will be an open-label, dose-escalation study to evaluate the safety and harmacology 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 colchicine binding mode, would offer a new approach to this target.