scholarly journals Thrombin-Receptor Antagonist Vorapaxar in Acute Coronary Syndromes

2012 ◽  
Vol 366 (1) ◽  
pp. 20-33 ◽  
Author(s):  
Pierluigi Tricoci ◽  
Zhen Huang ◽  
Claes Held ◽  
David J. Moliterno ◽  
Paul W. Armstrong ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Acute Coronary Syndromes ◽  
Thrombin Receptor ◽  
Coronary Syndromes ◽  
Thrombin Receptor Antagonist

Open Multicentre Study of the P 2T Receptor Antagonist AR-C69931MX Assessing Safety, Tolerability and Activity in Patients with Acute Coronary Syndromes

2001 ◽  
Vol 85 (03) ◽  
pp. 401-407 ◽  
Author(s):  
Keith Oldroyd ◽  
Robert Wilcox ◽  
Robert Storey ◽  
Keyword(s):  
Platelet Aggregation ◽  
Receptor Antagonist ◽  
Acute Coronary Syndromes ◽  
Plasma Concentrations ◽  
Antithrombotic Agent ◽  
Serious Adverse Events ◽  
Central Process ◽  
Impedance Aggregometry ◽  
Safety Parameters ◽  
Coronary Syndromes

SummaryPlatelet aggregation is the central process in the pathophysiology of acute coronary syndromes. ADP contributes to thrombosis by activating platelets, and AR-C69931MX is a specific antagonist of this process acting at the P 2T receptor. At 5 hospitals, 39 patients with unstable angina or non-Q wave myocardial infarction, who were receiving aspirin and heparin, were administered intravenous AR-C69931MX with stepped dose increments over 3 h to a plateau of either 2 μg/kg/min for 21 h (Part 1; n = 12) or up to 69 h (Part 2; n = 13) or 4 μg/kg/min for up to 69 h (Part 3: n = 14). Safety parameters, platelet aggregation (PA) induced by ADP 3 μmol/L (impedance aggregometry), bleeding time (BT) and plasma concentrations of AR-C69931XX were assessed. AR-C69931MX was well tolerated. 33 patients completed the study. There were no deaths at 30 days and no serious adverse events attributed to AR-C69931MX. Trivial bleeding (56%) was common. At 24 h, mean inhibition of PA was 96.0 ± 8.6, 94.9 ± 14.4 and 98.7 ± 2.1% and BT was 9.5 ± 8.4, 14.0 ± 9.7 and 16.0 ± 11.1 min for Parts 1, 2 and 3 respectively. At 1 h post-infusion, mean inhibition of PA was 36.2 ± 39.2, 20.7 ± 25.9 and 40.7 ± 36.7% respectively. 90% patients had a plasma half-life for AR-C69931XX of 9 min. In conclusion, AR-C69931MX is a potent, short-acting platelet ADP receptor antagonist suitable for further studies as an antithrombotic agent.

Development of Potent Thrombin Receptor Antagonist Peptides

1996 ◽  
Vol 39 (25) ◽  
pp. 4879-4887 ◽  
Author(s):  
Michael S. Bernatowicz ◽  
Clifford E. Klimas ◽  
Karen S. Hartl ◽  
Marianne Peluso ◽  
Nick J. Allegretto ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Thrombin Receptor ◽  
Antagonist Peptides ◽  
Thrombin Receptor Antagonist
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