Garadacimab  (Synonyms: CSL312)

Garadacimab (CSL312) is a first-in-class, fully human IgG4 monoclonal antibody targeting activated factor XII (FXIIa). Garadacimab has the potential for hereditary angioedema research^[1].

Human IgG4 lambda

Humanized

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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) plasma concentrations increased in a dose-dependent manner^[1].
Garadacimab has an inhibitory effect on FXII-mediated kallikrein activity. Furthermore, Garadacimab causes a clear dose-dependent prolongation of activated partial thromboplastin time (aPTT) with no associated effect on the prothrombin time^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

146500.00

2162134-62-3

Liquid

Colorless to light yellow

[Garadacimab]

Shipping with dry ice.

Please store the product under the recommended conditions in the Certificate of Analysis.

• 
  Human IgG4 lambda

• 
  Immobilized Factor FXIIa, Human can bind Garadacimab. The EC₅₀ for this effect is 12.81 ng/mL.

• [1]. Dipti Pawaskar, et al. Pharmacokinetic/pharmacodynamic modeling for dose selection for the first-in-human trial of the activated Factor XII inhibitor garadacimab (CSL312). Clin Transl Sci. 2022 Mar;15(3):709-720.  [Content Brief]

  [2]. Helen Cao, et al. Antibody-mediated inhibition of FXIIa blocks downstream bradykinin generation. J Allergy Clin Immunol. 2018 Oct;142(4):1355-1358.  [Content Brief]