Drug intelligence / Profile preview

FXII-uPAR abrogating peptides

Development stage
Preclinical
Lead developer
Case Western Reserve University
Modality
Peptides
Administration
Intravenous
01

Overview

FXII-uPAR abrogating peptides (also known as Combo) are a combination of three synthetic peptides (IPPWEAPK, DLAQCQTPTQAAPPTPVSPR, and LHVPLMPAQPAPPKPQPTTR) designed to selectively disrupt the interaction between coagulation factor XII (FXII) and the urokinase-type plasminogen activator receptor (uPAR). This interaction, which is zinc-dependent, occurs on the surface of activated neutrophils and drives thromboinflammation, neutrophil trafficking, and neutrophil extracellular trap (NET) formation via Akt2 phosphorylation. By blocking the FXII-uPAR signaling axis without compromising the enzymatic activity of activated FXII (FXIIa), these peptides attenuate thrombosis and inflammation without increasing bleeding risk. They are being investigated for the treatment of deep vein thrombosis (DVT), cancer-associated thrombosis (specifically ovarian cancer-associated thrombosis), sickle cell disease, and wound healing.

Other names
combination of IPP-DLA-LHV peptidesFXII-uPAR inhibitory peptidesIPP-DLA-LHV peptides
02

Targets

AKT2 (Rac-beta serine/threonine-protein kinase)F12 (Coagulation Factor XII)ITGB1 (Integrin beta-1)PLAUR (Urokinase plasminogen activator receptor)

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