Tigris in-licensed the exclusive worldwide rights to GGTI-2418 from Yale University and the University of South Florida.
Edmundo Muniz, president and CEO of Tigris, said: The filing of this investigational new drug application (IND) ahead of the scheduled date represents a major corporate achievement for the entire Tigris team.
Pending acceptance by the FDA, we plan to initiate a Phase I study of GGTI-2418 in two top Phase I cancer research centers 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.
According to the company, GGTI-2418 is a synthetic peptidomimetic inhibitor of geranylgeranyltransferase I that appears to induce apoptosis by downregulating several pivotal oncogenic and tumor survival pathways. GGTase I catalyzes the lipid posttranslational modification which is required for the function of Rho GTPases. 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 tumor suppressor Rb. GGTase I inhibitors also induce apoptosis by a mechanism involving downregulation of the expression of survivin and suppression of the activation of PI3K/Akt.