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PNB-081 is a small molecule cholecystokinin A (CCK-A) receptor antagonist being developed by PNB Vesper Life Sciences. Chemically characterized as an N-isobutyl-5-hydroxy-5-aryl-pyrrol-2-one compound, it is primarily targeted for the management of opioid addiction and the treatment of pancreatitis. By antagonizing the CCK1/CCK-A receptor, PNB-081 has been shown in preclinical studies to enhance the analgesic effects of opioids like morphine and tramadol while simultaneously preventing the development of opioid tolerance. In the context of pancreatitis, the drug aims to modulate the physiological role of cholecystokinin in pancreatic enzyme release. PNB-081 has completed preclinical IND-enabling studies in collaboration with the National Institute on Drug Abuse (NIDA) at the NIH.
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