Locus Pharma files first IND on cancer drug cadidate

Pennsylvlania, USA-based Locus Pharmaceuticals says that it has submitted an Investigational New Drug application to the Food and Drug Administration to begin a Phase I human clinical study of its lead compound, LP-261, an orally-administered small-molecule agent for the treatment of cancer.

LP-261 was developed by Locus using its proprietary computational drug design technologies. It is predicted to interact with tubulin at a unique binding site. In tumor cells, LP-261 induces growth arrest at the G2/M phase of cellular replication, resulting in programmed cell death (apoptosis). Approved tubulin targeting agents, such as the taxanes, are a highly effective class of cancer-killing agents, and such cytotoxics represent one of the largest markets in the pharmaceutical industry. The clinical limitations to these approved agents include intravenous delivery and multi-drug resistance.

The Phase I clinical study is designed to evaluate the safety and pharmacokinetic profile of LP-261 in patients with advanced metastatic tumors or blood cancers, as well as refractory cancer that has progressed despite previous chemotherapy. LP-261 has been shown preclinically to have 100% oral bioavailability in several animal species. Tumor response and blood levels of LP-261 will be assessed, and biomarkers of tubulin function, tumor cell division, and angiogenesis will be monitored, the company notes.