Drug intelligence / Profile preview

PEGSerp-1

Development stage
Preclinical
Lead developer
University of Florida
Modality
PEGylated Peptides → Modified Peptides → Peptides, Recombinant Proteins and Enzymes
Administration
Intravenous, Subcutaneous
01

Overview

PEGSerp-1 is a pegylated recombinant form of Serp-1, a 55 kDa serine protease inhibitor (serpin) derived from the Myxoma virus. It functions by irreversibly inhibiting key proteases in the inflammatory and coagulation cascades, specifically urokinase-type plasminogen activator (uPA), tissue-type plasminogen activator (tPA), and Factor Xa. By neutralizing these proteases, PEGSerp-1 modulates the migration of inflammatory cells, specifically reducing the infiltration of pro-inflammatory M1 macrophages and subsequent fibrotic tissue deposition. The pegylation of the Serp-1 protein enhances its pharmacokinetic profile by increasing its circulatory half-life and reducing potential immunogenicity compared to the native protein. PEGSerp-1 is primarily being investigated for the treatment of chronic inflammatory and fibrotic conditions, such as Duchenne muscular dystrophy (DMD), where it has demonstrated the ability to reduce diaphragm fibrosis and promote muscle fiber regeneration in preclinical models. While the non-pegylated Serp-1 has previously been evaluated in Phase 2 clinical trials for acute coronary syndrome, PEGSerp-1 represents a long-acting formulation designed for chronic therapeutic applications.

Other names
Pegylated Serp-1PEG-Serp-1PEG-Serp1PEG-Serp 1
02

Targets

F10 (Factor Xa)F2 (Thrombin)PLAU (uPA)PLAT (Tissue-type plasminogen activator)C1S (Complement component 1s subcomponent serine protease)PLG (Plasminogen)

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