Jenrin Discovery’s IND Application for Its Peripherally Restricted Cannabinoid-1 Receptor Inverse Agonist NASH Compound Was Cleared by the FDA to Begin Phase I Clinical Trials

CHADDS FORD, Pa.--(BUSINESS WIRE)-- Jenrin Discovery has announced today that the FDA has cleared the Investigational New Drug (IND) Application for JD5037, Jenrin’s novel peripherally restricted (PR) CB₁ receptor inverse agonist, to begin Phase 1 clinical trials. JD5037, to be developed to treat nonalcoholic steatohepatitis (NASH), was specifically designed to minimize blood-brain barrier penetration and brain receptor occupancy (RO) that mediates the neuropsychiatric liability associated with first-generation brain penetrant CB₁ receptor blockers. Jenrin has developed JD5037 in part through collaboration with scientists at the National Institutes of Health (NIH) and financial support from the NIH Bridging Interventional Development Gaps (BriDGs) program.

JD5037 has been shown to beneficially modulate the metabolic parameters associated Type 2 diabetes, obesity and associated liver and kidney diseases in a variety of animal models. However, unlike earlier agents in this class, pre-clinical studies in both rodents (PET – RO, NIH) and primates (CSF levels) support an absence of pharmacologically relevant compound in the brain. In addition, JD5037 may affect collagen synthesis in hepatic stellate cells making it useful for the treatment of NASH-related fibrosis. JD5037 also has high potency in inhibiting β–arrestin2 activation, another factor in fibrotic disease development. These properties, along with its beneficial effects on metabolic processes, indicate JD5037 may be able to suppress the progression of hepatic fibrosis and provide efficacious therapy for the treatment of NASH.

“Compounds with a unique pharmacological profile impacting the metabolic processes associated with non-alcoholic fatty liver disease (NAFLD), as well as factors associated with the development and progression of fibrosis, provide the multi-hit approach that many feel will be necessary in treating advanced liver disease such as NASH,” said Bob Chorvat, Ph.D., CSO of Jenrin Discovery. “Whether a stand-alone drug, or part of a multi-factorial therapeutic approach, JD5037 has the potential to play a significant role in treating this unmet medical need.”

About Jenrin Discovery, Inc. (www.jenrindiscovery.com) -- Founded in 2005, Jenrin Discovery is a privately-held company developing proprietary, small molecule drugs designed to selectively target peripheral tissues. These new chemical entities retain the pharmacological activity and other drug-like properties of the parent compound, but carry little or no risk of neuropsychiatric effects, thus offering a potentially safer alternative to the original agents.

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