BI 1356225

BI 1356225 is an orally active small molecule inhibitor of ghrelin O-acyltransferase (GOAT), developed by Boehringer Ingelheim. Its primary mechanism is inhibition of acetyltransferase activity, specifically targeting the GOAT enzyme, which plays a key role in the acylation and activation of ghrelin, a hormone involved in appetite regulation and energy homeostasis. The drug has been investigated for obesity and opioid-related disorders. In clinical studies, BI 1356225 significantly reduced acylated ghrelin concentrations but did not show clinically meaningful effects on body weight or appetite over short-term treatment periods. Current development focuses on its potential to improve impulse control in men with opioid use disorder who are maintained on buprenorphine[1][2][4][6][8].