BIA 10-2474

BIA 10-2474 is a potent FAAH inhibitor with IC50s of 50-70 μg/kg (i.p.) in various brain regions; also inhibits several lipases that are not targeted by PF04457845, produces substantial alterations in lipid networks in human cortical neurons.Pain Phase 1 Discontinued (In Vitro) :ExVivo: BIA 10-2474 proves to be a potent FAAH inhibitor with IC50s of 50-70mg/kg (i.p.) in various brain regions. IC50 values for brain regions are 52 (cerebellum), 67 (rest of brain), 68 (cortex), and 71 mg/kg (hypothalamus) . (In Vivo) :In January 2016, severe adverse events (SAE) occurs in the Phase I clinical trial using the drug BIA 10-2474 including one death. The possibilities for failure of trials such as off-target effect, dose calculation, unexpected immune response, species variation, and cumulative dose toxicity would be sought.