Garadacimab (CSL312) is a potent whole-human IgG4 monoclonal antibody targeting activation factor XII (FXIIa). Garadacimab can be used to study hereditary angioedema.

β-FXIIa:140 pM(Kd)

Garadacimab (CSL312) demonstrates high affinity to activated βFXIIa with a KD of 140 pM. In an activated partial thromboplastin time (aPTT) assay with human plasma, Garadacimab exhibits potency. Notably, it displays high selectivity over a panel of relevant human serine proteases, including FVIIa, FIXa, FXa, FXIa, kallikrein, tissue plasminogen activator, activated protein C, and urokinase plasminogen activator[2].

In male and female cynomolgus monkeys, Garadacimab (0.5, 1, and 3 mg/kg i.v. and 6 and 20 mg/kg s.c. over 8 weeks) shows a dose-dependent increase in plasma concentrations[1]. Garadacimab exhibits an inhibitory effect on FXII-mediated kallikrein activity. Moreover, it induces a clear dose-dependent prolongation of activated partial thromboplastin time (aPTT) with no associated effect on the prothrombin time[1].