Tigris Pharmaceuticals, Inc., a privately held drug development company, announced that it has filed an Investigational New Drug (IND) application with the US Food and Drug Administration (FDA) for GGTI-2418, a novel anticancer compound. GGTI-2418 is a synthetic peptidomimetic inhibitor of geranylgeranyltransferase I (GGTase I) that appears to induce apoptosis by down regulating several pivotal oncogenic and tumour survival pathways.

"The filing of this IND ahead of the scheduled date represents a major corporate achievement for the entire Tigris team," said Edmundo Muniz, M.D., Ph.D., president and chief executive officer of Tigris. "Pending acceptance by the FDA, we plan to initiate a phase 1 study of GGTI-2418 in two top phase I cancer research centres in the first half of 2009. This will be the first geranylgeranyltransferase inhibitor in human clinical trials in this well-validated pathway and represents an important advancement in identifying novel approaches to treat cancer."

"The submission of this IND marks an extremely important and exciting time in the field of geranylgeranylation inhibitors. I look forward to the fruitful translation of our preclinical work to target patients whose tumours harbour aberrant signal transduction pathways most likely to respond to GGTI-2418," stated Said M. Sebti, Ph.D., director of the drug discovery program at the Moffitt Cancer Center and co-inventor of GGTI-2418. "This is a most important and gratifying step in the development of GGTI-2418 as a novel treatment for the devastating effects of cancer," noted Andrew Hamilton, Ph.D., Professor of Chemistry at Yale University and co-inventor of GGTI-2418.

Tigris in-licensed the exclusive worldwide rights to GGTI-2418 from Yale University and the University of South Florida.

GGTI-2418 is a synthetic peptidomimetic inhibitor of geranylgeranyltransferase I (GGTase I) that appears to induce apoptosis by down regulating several pivotal oncogenic and tumour survival pathways. GGTase I catalyzes the lipid posttranslational modification which is required for the function of Rho GTPases (frequently found aberrantly activated in human cancer). GGTase I inhibitors block Rho function in cancer cells and induce a G1 phase cell cycle arrest by a mechanism involving induction of the CDK inhibitors p21waf and p27kip, CDK2 and CDK4 inhibition and hypophoshorylation of the tumour suppressor Rb. GGTase I inhibitors also induce apoptosis by a mechanism involving down regulation of the expression of surviving and suppression of the activation of PI3K/Akt.

Tigris Pharmaceuticals, Inc. is a privately held biopharmaceutical company that develops therapeutic technologies, using a translational research approach, for use in oncology and other areas of unmet medical need. Tigris' mission is to efficiently move its existing and future technologies through the various stages of clinical development in order to meet patients' needs for safe and effective treatments of human illnesses.