Introduction M8891 is a selective and reversible inhibitor of methionine aminopeptidase 2 (MetAP2). We describe translational research to define the target pharmacokinetics (PK) of M8891 and associated pharmacodynamic (PD) levels, which were used to support efficacious dose selection in humans. Methods In vitro and in vivo PK characteristics were investigated in animal species, and data integrated using in vitro–in vivo correl...