Drug intelligence / Profile preview

c1-esterase inhibitor (Sanquin)

Development stage
Approved
Lead developer
Grifols
Modality
Recombinant Proteins and Enzymes
Administration
Intravenous
01

Overview

Human C1-inhibitor (C1-INH) is a plasma-derived serine protease inhibitor (serpin) that serves as a critical regulator of the classical complement pathway, the contact-kinin system, and the intrinsic coagulation cascade. It functions by irreversibly binding to and inactivating several target proteases, including C1r, C1s, plasma kallikrein, and activated factor XII. While primarily indicated for the treatment and prophylaxis of hereditary angioedema (HAE) to prevent excessive bradykinin production, it has been investigated for other inflammatory conditions. In the CAST trial (NCT03051698), human C1-inhibitor (marketed as Cetor by Sanquin) was evaluated by the Academic Medical Center, University of Amsterdam, for its potential to modulate bronchial inflammation and coagulation in patients with allergic asthma. However, the Phase 4 mechanistic study was terminated after an interim analysis failed to demonstrate significant differences between the treatment and control groups.

Brand names
CetorBerinertCinryzeHaegarda
Other names
human C1-inhibitorC1-INHC-1-INHC 1-INHplasma-derived C1-inhibitor
02

Targets

MASP2 (Mannan-binding lectin-associated serine protease 2)MASP1 (MASP-1)FXIIa (Coagulation Factor XIIa)C1S (Complement component 1s subcomponent serine protease)Factor XIaC1R (Complement component 1r subcomponent)KLKB1 (Plasma kallikrein)

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