Proglumide

Proglumide is an orally bioavailable small molecule drug that acts primarily as a cholecystokinin (CCK) receptor antagonist, blocking both cholecystokinin receptor type A (CCK-AR; CCK1-R) and gastrin/cholecystokinin type B receptor (CCK-BR; CCK2-R). It reduces gastric acid secretion and gastrointestinal motility, and has been used in the treatment of peptic ulcer disease. Proglumide also exhibits potential antineoplastic activity, with studies showing it can reverse liver fibrosis and decrease the incidence of hepatocellular carcinoma in animal models. Additionally, it may act as a partial agonist at the farnesoid X receptor (FXR), which could contribute to its effects on nonalcoholic steatohepatitis (NASH). An interesting property of proglumide is its ability to enhance opioid analgesia and reduce opioid tolerance, possibly by modulating neural pathways involved in expectation and placebo response.

Brand names

Milid

Other names

proglumide