Drug intelligence / Profile preview

PZ-128

Development stage
Phase 2
Lead developer
Tufts Medical Center
Modality
Modified Peptides → Peptides, Small Molecules, Recombinant Proteins and Enzymes
Administration
Intravenous
01

Overview

PZ-128 is a first-in-class pepducin inhibitor of protease-activated receptor 1 (PAR1), developed as an antiplatelet agent for patients with coronary artery disease and acute coronary syndromes undergoing percutaneous coronary intervention. Pepducins are lipidated peptides that target the cytoplasmic surface of their cognate G protein-coupled receptors. PZ-128 acts by reversibly inhibiting PAR1 on platelets and other vascular cells through a novel intracellular mechanism at the receptor–G protein interface. This results in rapid, specific, dose-dependent, and reversible inhibition of platelet activation and aggregation without significant effects on other platelet receptors or coagulation parameters. In clinical trials (up to phase 2), it has shown potential benefit in reducing myocardial injury risk during cardiac interventions while maintaining a favorable safety profile[1][6][7][8].

Other names
Palmitate-kksralf-NH2Palmitate-kksralf-NH-2Palmitate-kksralf-NH 2
02

Targets

F2R (Protease-activated receptor 1)

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