Team describes off-target effects of Bial's FAAH inhibitor

In a paper published in Science, researchers characterized off-target activities of fatty acid amide hydrolase (FAAH) inhibitor BIA 10-2474 that they say may have played a role in the compound’s clinical neurotoxicity that led to the death of one participant in a Phase I trial, and caused brain damage in others. The group said the compound inhibited lipases another FAAH inhibitor did not.

Bial-Portela & Ca. S.A. (S. Mamede do Coronado, Portugal) was developing BIA 10-2474 to treat pain. In January 2016, Bial-Portela halted its Phase I study in France after six healthy volunteers were hospitalized with serious "neurological troubles," including one who was brain-dead (see BioCentury Extra, Jan. 15, 2016)...