Jenrin’s most advanced program targets peripheral CB1 receptors for the treatment of metabolic disorders. Because of the risk of psychiatric side effects, all development programs associated with brain-penetrant CB1 blockers were halted, and the only marketed product (rimonabant) was withdrawn. In addition to producing weight loss, these brain-penetrant CB1 inverse agonists improve lipid levels and glycemic control, increase fat metabolism, and decrease fatty liver via interactions with CB1 receptors outside the brain.
Thus, the Jenrin peripherally selective (PS) CB1 receptor blocker strategy captures the beneficial properties these agents exert through blockade of CB1 receptors in peripheral tissues (e.g., liver, muscle, adipose, pancreas) with minimal or no CNS penetration, and an absence psychiatric and neurologic liabilities.
Jenrin has established an extensive PS CB1 receptor blocker patent estate with applications covering six distinct chemical series. By using clinically advanced CB1 blockers as starting points for our drug discovery efforts, proprietary high affinity lead candidates with functionality to limit or eliminate brain exposure have been identified in three of these series. The Jenrin strategy capitalizes on the years of medicinal chemistry effort by others to optimize the efficacy of the original drug, significantly shortening discovery timelines while improving safety.JD5037, Jenrin’s lead compound, has been shown in animals fed a high-fat diet to reduce body weight, decrease fatty liver and lower serum triglyceride levels while improving glucose tolerance and insulin resistance – all metabolic factors associated with NASH. Moreover, the ability of CB1 inverse agonists / JD5037 to:
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