The First Potential Kappa Opioid Receptor Agonist: CR845

Cara Therapeutics is developing the first peripherally acting kappa opioid receptor agonist (KORA) called CR845. CR845 is a potent peripheral kappa opioid receptor agonist with high selectivity over other opioid receptors in the body. The degree of kappa receptor selectivity displayed by CR845 ranks as best-in-class compared to all other previously developed compounds for this therapeutic target. Moreover, CR845 displayed no significant affinity for any other non-opioid known receptors.

CR845 exhibits potent analgesic, anti-pruritic (anti-itch) and anti-inflammatory properties in both human and animals. Since CR845 is intrinsically poor at penetrating the blood-brain barrier, it has shown to produce little to no CNS-mediated side effects that one sees with traditional CNS-acting mu opioids like nausea/vomiting, sedation, respiratory depression, abuse, addiction or euphoria.