Regen BioPharma has initiated in vivo and ex vivo assessments to determine the effects of some of the company's NR2F6 small molecule agonists in live rats and in tissues derived from humans and rats. Key attributes that are being measured include pH, plasma and liver microsomal stability, along with pharmacokinetics.
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 agonists which should suppress the immune system in diseases where the immune system is over-activated, such as autoimmunity. The program also aims to identify antagonists of NR2F6 in an effort to unleash the cancer-killing potential of a patient's own immune system.
"Initial studies are quite positive. Our compounds are stable at pH 2 and 7, stable in rat and human plasma, additionally one of our compounds shows very nice pharmacokinetics with an oral or intravenous half-life of about 2.5 hrs," said Harry Lander, Ph.D., MBA, President and Chief Scientific Officer of Regen. "Getting this data early in the process informs us of any liabilities the compounds may have which we would need to address via medicinal chemistry. So far, these molecules look like they will be orally deliverable and will not require too much more tweaking before we can start testing them for efficacy."