Qualigen, Inc., and the University of Louisville (UofL) today announced that Qualigen has entered into a Sponsored Research Agreement (SRA) with UofL for development of several small-molecule RAS Inhibitor drug candidates. Under the terms of this Sponsored Research Agreement, Qualigen assumed funding responsibility for this program from April 1, 2019 through September 30, 2020.
RAS is the most common oncogene in human cancer. Activating mutations in one of the three human RAS gene isoforms (KRAS, HRAS, or NRAS) are present in about one-fourth of all cancers. As an example, mutant KRAS is found in 98% of all pancreatic ductal adenocarcinomas, 52% of all colon cancers, and 32% of all lung adenocarcinoma. Every year in the U.S., these three mutant KRAS associated cancers are diagnosed in more than 170,000 people, resulting in more than 120,000 deaths. There are no FDA-approved direct RAS protein inhibitors currently available. Drugs that target downstream signaling of RAS are available but have shown disappointing clinical activity, most likely because RAS is a “hub” that activates multiple effectors and blocking any single pathway (or even two) will be ineffective. RAS is a G-protein that works as a switch, toggling between “on” and “off” when bound to guanosine nucleotides, GTP or GDP. The RAS mutations found in cancer cause this protein to be turned on (i.e. bound to GTP) most of the time. Most drug targets are proteins that have a well-defined “pocket” that can be targeted by small molecules, as with enzymes (substrate binding site) or kinases (ATP binding site). However, RAS lacks such pockets and thus is more difficult to target directly, but the UofL team has been able to develop small molecules that are protein-protein interaction (PPI) inhibitors that block the binding of RAS to its effector proteins.
“We are excited about the possibility of adding a small molecule RAS Inhibitor to our portfolio of anticancer drug technologies. This technology is synergistic with our other cancer therapeutics platforms and will expand our future product pipeline,” noted Michael S. Poirier, Chairman, CEO and President of Qualigen. “We are pleased to partner with UofL to continue the innovative work of Dr. Geoffrey Clark, Dr. John Trent and their colleagues at the University of Louisville. We believe that this research will result in a powerful new tool in the fight against cancer.”
This technology was developed at UofL with key support from several robust programs, including UofL’s ExCITE program, a National Institutes of Health Research Evaluation and Commercialization Hub (REACH). These programs drive the translation of innovative research from UofL’s campus to the marketplace, leading to licensing through the university’s Commercialization EPI-Center.
“We are excited to work with Qualigen on the product development of our small molecule RAS Inhibitor drug to fight cancer,” said Dr. Allen Morris, EPI-Center’s director. “This is the kind of outcome UofL seeks in its translational efforts – working closely with industry to get our cutting-edge research to market.”