Garadacimab  (Synonyms: 加达西单抗; 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) 对活化的 βFXIIa 表现出高亲和力，K_D 为 140 pM，并在人血浆的活化部分凝血活酶时间 (aPTT) 测定中显示出效力。Garadacimab 对一组相关的人丝氨酸蛋白酶（FVIIa、FIXa、FXa、FXIa、激肽释放酶、组织纤溶酶原激活剂、活化蛋白 C 和尿激酶纤溶酶原激活剂）显示出高选择性^[2]。

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

在雄性和雌性食蟹猴中，Garadacimab（0.5、1 和 3 mg/kg i.v. 以及 6 和 20 mg/kg s.c. 超过 8 周）血浆浓度以剂量依赖性方式增加^[1]。
Garadacimab 对 FXII 介导的激肽释放酶活性具有抑制作用。 此外，Garadacimab 导致活化部分凝血活酶时间 (aPTT) 明显剂量依赖性延长，而对凝血酶原时间没有相关影响^[1]。

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

2162134-62-3

液体

Colorless to light yellow

加达西单抗

Shipping with dry ice.

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

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  Human IgG4 lambda

• [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]