QUICK SEARCH:   [advanced] Author: Keyword(s): Year:  Vol:  Page:

This Article Résumé Extracto Full Text PDF Alert me when this article is cited Alert me if a correction is posted Services Email this article to a friend Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Articles Ahead of Print [Order Reprint] Citing Articles Citing Articles via Google Scholar Google Scholar Articles by Scott, D. M. Articles by Parra, D. Search for Related Content PubMed PubMed Citation Articles by Scott, D. M. Articles by Parra, D.

NEW DRUG DEVELOPMENTS

P2Y₁₂ Inhibitors in Cardiovascular Disease: Focus on Prasugrel

Director of Experiential Programs, Institutional Practice; Assistant Professor of Pharmacy Practice, Lloyd L Gregory School of Pharmacy, Palm Beach Atlantic University, West Palm Beach, FL

Rhonda M Norwood, PharmD

Assistant Professor of Pharmacy Practice, Lloyd L Gregory School of Pharmacy, Palm Beach Atlantic University

David Parra, PharmD BCPS

Clinical Pharmacy Specialist—Cardiology, Veterans Affairs Medical Center, West Palm Beach, FL; Clinical Assistant Professor, Department of Experimental and Clinical Pharmacology, College of Pharmacy, University of Minnesota, Minneapolis, MN

Reprints: Dr. Scott, Lloyd L Gregory School of Pharmacy, Palm Beach Atlantic University, PO Box 24708, West Palm Beach, FL 33416, fax 561/803-2703, day_scott{at}pba.edu

OBJECTIVE: To review the literature describing the pharmacology, pharmacokinetic properties, efficacy, and adverse effects of prasugrel, a new thienopyridine.

DATA SOURCES: A literature search was conducted (1966–November 2008) of the MEDLINE, Current Contents, EMBASE, and International Pharmaceutical Abstract databases using the key words prasugrel, CS-747, LY640315, and P2Y₁₂. Bibliographies of identified literature were also reviewed for additional references.

STUDY SELECTION AND DATA EXTRACTION: All reports published in English that evaluated prasugrel (or its chemical synonyms) were reviewed. Abstracts without subsequently published reports were excluded.

DATA SYNTHESIS: Given the high rate of recurrent coronary events despite current antiplatelet therapies, agents with potentially greater efficacy are under investigation. Prasugrel is a novel thienopyridine prodrug that is rapidly metabolized to its active platelet-inhibitory metabolite (R-138727) and exerts antiplatelet activity through antagonism of P2Y₁₂ receptors. Prasugrel is very similar in structure and mechanism of action to clopidogrel, as they both possess a methoxycarbonyl group that provides increased pharmacologic activity and an improved hematologic safety profile when compared with ticlopidine. In addition, when compared with clopidogrel, prasugrel demonstrates greater potency and less interpatient variability in the inhibition of platelet aggregation, less in vitro hyporesponsiveness, and, in patients with acute coronary syndromes, a reduced rate of ischemic events. However, this reduction in ischemic events was accompanied by an increased risk of major and fatal bleeding.

CONCLUSIONS: Prasugrel appears to be a promising antiplatelet agent, with emerging clinical data in direct comparison with clopidogrel supporting its role in reducing recurrent ischemic events. Further studies are needed to evaluate the safety and efficacy of prasugrel across various patient populations and clinical scenarios.

Key Words: CS-747, LY640315, P2Y₁₂, prasugrel, thienopyridine

Published Online, December 2, 2008. www.theannals.com, DOI 10.1345/aph.1G726

THIS ARTICLE IS APPROVED FOR CONTINUING EDUCATION CREDIT
ACPE UNIVERSAL PROGRAM NUMBER: 407-000-09-001-H01-P