Regen BioPharma sees success in Its pre-clinical small molecule optimization program for NR2F6

The company's small molecule drug program is aimed at treating cancer and autoimmune diseases.

Regen BioPharma has completed the first phase of its small molecule optimization program, which involved synthesizing more than 40 analogues of its initial lead compounds (RG-NA01, RG-NA02, RG-NI01 and RG-NI02). The compounds synthesized consist of activators (RG-NA01 and RG-NA02) and inhibitors (RG-NI01 and RG-NI02) of NR2F6 and were identified using Regen's patented screening methodology and unique chemical libraries.

With the crucial first phase completed the company, along with ChemDiv, can move forward with the optimization process, which involves introducing the synthesized compound analogues to cells specifically designed to respond to NR2F6 agonists and learning more about their potency.

The NR2F6 nuclear receptor has been identified as a potentially very important immune cell inhibitor (an immune checkpoint) and cancer stem cell differentiator. The NR2F6 program at Regen aims to identify antagonists of NR2F6 in an effort to unleash the cancer-killing potential of a patient's own immune system, as well as identifying agonists which should suppress the immune system in diseases where the immune system is over-activated, such as autoimmunity (e.g.: arthritis).

"The ChemDiv team has synthesized more than 40 analogues of our initial small molecules and has begun screening them for activity. We are excited that several of these compounds have dose-dependent activity in our cellular assay," says Harry Lander, President and Chief Scientific Officer of Regen. "We are currently evaluating the relationship between the structure of the compounds and their activity. By performing careful and thoughtful medicinal chemistry, we expect to be in a strong position in a few months, in terms of having a well-understood optimized activator and inhibitor of NR2F6."

David Koos, Regen BioPharma's Chairman & CEO noted: "We have identified compounds that will likely cause the body's own immune system to fight cancer and autoimmune diseases, such as arthritis, by manipulating the immune checkpoint NR2F6. A key differentiator for Regen is being able to deliver these therapies through small molecule treatments (e.g.; pill form), which should produce an easier and more comfortable approach for patients, leading to fewer and less severe side effects than currently used therapies."