Cell-Penetrating Pepducin Therapy Targeting PAR1 in Subjects With Coronary Artery Disease

• Published in: Arteriosclerosis, thrombosis, and vascular biology Vol. 36; no. 1; pp. 189 - 197
• Main Authors: Gurbel, Paul A., Bliden, Kevin P., Turner, Susan E., Tantry, Udaya S., Gesheff, Martin G., Barr, Travis P., Covic, Lidija, Kuliopulos, Athan
• Format: Journal Article
• Language: English
• Published: United States American Heart Association, Inc 01.01.2016
• Subjects: Adult; Aged; Blood Platelets - drug effects; Blood Platelets - metabolism; Cell-Penetrating Peptides - administration & dosage; Cell-Penetrating Peptides - adverse effects; Cell-Penetrating Peptides - pharmacokinetics; Coronary Artery Disease - blood; Coronary Artery Disease - diagnosis; Coronary Artery Disease - therapy; Dose-Response Relationship, Drug; Female; Half-Life; Humans; Infusions, Intravenous; Lipopeptides - administration & dosage; Lipopeptides - adverse effects; Lipopeptides - pharmacokinetics; Male; Middle Aged; Percutaneous Coronary Intervention - adverse effects; Platelet Aggregation - drug effects; Platelet Aggregation Inhibitors - administration & dosage; Platelet Aggregation Inhibitors - adverse effects; Platelet Aggregation Inhibitors - pharmacokinetics; Platelet Function Tests; Receptor, PAR-1 - antagonists & inhibitors; Receptor, PAR-1 - metabolism; Treatment Outcome; coronary artery disease; collagen; aspirin; risk factors; lipopeptides

OBJECTIVE—Pepducins are membrane-tethered, cell-penetrating lipopeptides that target the cytoplasmic surface of their cognate receptor. Here, we report the first human use of a protease-activated receptor-1–based pepducin, which is intended as an antiplatelet agent to prevent ischemic complications...