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Empasiprubart

Product NameEmpasiprubart
CAS2579031-19-7
MF
MW0
EINECS
MOL FileMol File

Chemical Properties

form	Liquid
color	Colorless to light yellow

Usage And Synthesis

Uses

Empasiprubar (ARGX-117) is a humanized inhibitory monoclonal antibody targeting complement C2. Empasiprubar binds to the Sushi-2 domain of C2, preventing the formation of C3 pre convertase and inhibiting the activation of classical and lectin pathways upstream of C3 activation. Empasiprubar can prevent complement mediated autoimmune hemolytic anemia and antibody mediated organ transplant rejection. Empasiprubar can prevent neuroglial lymphoconjunctival injury in GM1 antibody mediated mouse models[1][2].

in vivo

Empasiprubart (0.5-30 mg/kg; once daily; 60 days; i.v.) targets the classical pathway (CP) and lectin pathway (LP) inhibition in crab eating macaques, without affecting the alternative pathway (AP)^[1]. Empasiprubart (200 mg/kg; once; i.v.) can prevent neuroglial lymphoconjunctival injury in GM1 antibody mediated mouse models^[2].

Animal Model:	Cynomolgus monkeys^[1].
Dosage:	0.5-30 mg/kg
Administration:	Intravenous injection (i.v.); once daily; 60 days
Result:	Reduced free C2 levels and classical pathway activity.

Animal Model:	Schwann cell nodal membrane injury mice model^[2].
Dosage:	200 mg/kg
Administration:	Intravenous injection (i.v.); once
Result:	Attenuated injury to paranodal proteins at the node of Ranvier and improves respiratory function in vivo Schwann cell nodal membrane injury models.

References

[1] Van de Walle I, et al. ARGX-117, a therapeutic complement inhibiting antibody targeting C2. J Allergy Clin Immunol. 2021 Apr;147(4):1420-1429.e7. DOI:10.1016/j.jaci.2020.08.028
[2] Campbell CI, et al. Complement inhibition prevents glial nodal membrane injury in a GM1 antibody-mediated mouse model. Brain Commun. 2022 Nov 23;4(6):fcac306. DOI:10.1093/braincomms/fcac306
[3] Budding K, et al. Anti-C2 Antibody ARGX-117 Inhibits Complement in a Disease Model for Multifocal Motor Neuropathy. Neurol Neuroimmunol Neuroinflamm. 2021 Nov 10;9(1):e1107. DOI:10.1212/NXI.0000000000001107

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