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The Rationale for and Clinical Pharmacology of Prasugrel 5 mg

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Abstract

Prasugrel is a third-generation thienopyridine platelet P2Y12 adenosine diphosphate (ADP) receptor antagonist administered with aspirin for the treatment of patients with acute coronary syndrome (ACS) with planned percutaneous coronary intervention. Prasugrel is administered periprocedurally at an oral loading dose of 60 mg followed by daily maintenance doses (MDs) of 10 mg for most patients and 5 mg for patients weighing <60 kg or aged ≥75 years. Data from a prasugrel phase III study, TRITON-TIMI 38, suggested that a lower MD might be more suitable for patients weighing <60 kg or aged ≥75 years; subsequent pharmacokinetic and pharmacodynamic studies have indicated that prasugrel 5 mg reduced platelet reactivity in these populations to an extent similar to that of prasugrel 10 mg in heavier or younger patients. Clinical experience with prasugrel 5 mg is limited, and additional studies are needed to verify the clinical efficacy and safety of this dose in these challenging populations.

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Acknowledgements

Appreciation is expressed to Chris Konkoy, Ph.D. of Eli Lilly and Company and Tamara Ball, MD of inVentiv Health for editorial assistance.

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Authors and Affiliations

  1. Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, 46285, USA

    Joseph A. Jakubowski, David S. Small & Kenneth J. Winters

  2. Department of Cardiology, Lund University, Lund, Sweden

    David Erlinge

  3. Department of Cardiology, Attikon University Hospital, National and Capodistrian University of Athens Medical School, Athens, Greece

    Dimitrios Alexopoulos

  4. Sinai Center for Thrombosis Research, Baltimore, MD, USA

    Paul A. Gurbel

  5. Cardiovascular Research Center at University of Florida College of Medicine-Jacksonville, Jacksonville, FL, USA

    Dominick J. Angiolillo

Authors
  1. Joseph A. Jakubowski
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  2. David Erlinge
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  3. Dimitrios Alexopoulos
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  4. David S. Small
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  5. Kenneth J. Winters
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  6. Paul A. Gurbel
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  7. Dominick J. Angiolillo
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Corresponding author

Correspondence to Joseph A. Jakubowski.

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Disclosures

Dr. Erlinge: Speaker honoraria: Daiichi Sankyo Company, Ltd., Eli Lilly and Company, AstraZeneca; Advisory board: AstraZeneca, Eli Lilly and Company, Merck. Dr. Alexopoulos: Speaker honoraria: AstraZeneca; Advisory Board: AstraZeneca, Boeringer Ingelheim, Bayer. Dr. Gurbel: Consultant: Daiichi Sankyo, Eli Lilly and Company, Bayer, AstraZeneca, Boehringer, Merck and Co., CSL, Janssen, and New Haven Pharmaceuticals; Grants: NIH, Daiichi Sankyo, Merck, New Haven Pharmaceuticals, Haemonetics, Sinnowa, Coramed, and Duke Clinical Research Institute; Patents: in the areas of personalized antiplatelet therapy and interventional cardiology. Dr. Angiolillo: Consulting fee or honorarium: Bayer, Amgen, Pfizer, Sanofi, Daiichi Sankyo, Inc, Eli Lilly and Company, The Medicines Company, AstraZeneca, Merck, Abbott Vascular and PLx Pharma; Review activities: CeloNova, Johnson & Johnson, and St. Jude Medical. Institution; Grants: Glaxo-Smith-Kline, Daiichi Sankyo, Inc, Eli Lilly and Company, The Medicines Company, AstraZeneca, Janssen Pharmaceuticals, Inc., Osprey Medical, Inc., Novartis, CSL Behring, and Gilead. Drs. Jakubowski, Small, and Winters are employees and minor shareholders of Eli Lilly and Company.

Funding

This review was funded by Daiichi Sankyo Company, Ltd. and Eli Lilly and Company.

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Jakubowski, J.A., Erlinge, D., Alexopoulos, D. et al. The Rationale for and Clinical Pharmacology of Prasugrel 5 mg. Am J Cardiovasc Drugs 17, 109–121 (2017). https://doi.org/10.1007/s40256-016-0202-3

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  • DOI: https://doi.org/10.1007/s40256-016-0202-3

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