Fasitibant chloride (MEN16132 free base) is a potent and specific nonpeptide antagonist of the bradykinin B2 receptor (B2R), effectively reducing joint pain and mitigating joint edema in a rat model of Carrageenan-induced arthritis.

Fasitibant chloride (MEN16132 free base; 1 μM; pre-treatment 30 min before BK) consistently reduces FGF-2 expression and diminishes BK-induced FGFR-1 phosphorylation without affecting FGFR-2 activity in HUVECs, also impeding the phosphorylation of FRSα, ERK1/2, and STAT3 but not AKT. In a cell viability assay on HUVECs, it demonstrated the same reduction in FGF-2 expression and decrease in BK-induced FGFR-1 phosphorylation.

Fasitibant chloride (MEN16132 free base; 100 μg per knee; injected into the knee 30 minutes before λ-carrageenan) effectively reduces carrageenan-induced joint pain and knee joint edema by 40-45% in male Wistar rats weighing 250-300 g[1]. The treatment also significantly decreases neutrophil infiltration in the synovium by approximately 60% and prostaglandin release by around 30%, showcasing potent anti-inflammatory and analgesic properties.