Figure 5

The effect of BR103354 on FAP inhibition and endogenous intact FGF21 levels in non-human primates. (a) IC50 values of BR103354 using serum FAP of mice, monkeys, and humans were determined. (b) Normal cynomolgus monkeys were treated with BR103354 by intranasal injection, and blood was collected at the indicated time points. The plasma concentration of BR103354 was quantified by LC–MS/MS, and plasma FAP activity was measured by fluorometric assay using AMC substrate. Intact FGF21 levels in plasma were measured by ELISA.