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Btk Inhibitors as First Oral Atherothrombosis-Selective Antiplatelet Drugs?

Authors
  • Busygina, Kristina1
  • Denzinger, Viola1
  • Bernlochner, Isabell2
  • Weber, Christian1, 3, 4
  • Lorenz, Reinhard1
  • Siess, Wolfgang1, 3
  • 1 Institute for Prevention of Cardiovascular Diseases, LMU (Ludwig-Maximilians University Munich), Munich, Germany. , (Germany)
  • 2 Medizinische Klinik und Poliklinik I, Klinikum rechts der Isar, Medizinische Fakultät, Technische Universität München, Munich, Germany. , (Germany)
  • 3 DZHK (German Centre for Cardiovascular Research), partner site Munich Heart Alliance, Munich, Germany. , (Germany)
  • 4 Department of Biochemistry, Cardiovascular Research Institute Maastricht (CARIM), Maastricht University, Maastricht, The Netherlands. , (Netherlands)
Type
Published Article
Journal
Thrombosis and Haemostasis
Publisher
Georg Thieme Verlag KG
Publication Date
Aug 01, 2019
Volume
119
Issue
8
Pages
1212–1221
Identifiers
DOI: 10.1055/s-0039-1687877
PMID: 31087308
Source
Medline
Language
English
License
Unknown

Abstract

Bruton's tyrosine kinase (Btk) is essential for B cell differentiation and proliferation, but also platelets express Btk. Patients with X-linked agammaglobulinemia due to hereditary Btk deficiency do not show bleeding, but a mild bleeding tendency is observed in high dose therapy of B-cell malignancies with ibrutinib and novel second-generation irreversible Btk inhibitors (acalabrutinib and ONO/GS-4059). This review discusses recent studies that may explain this apparent paradox and gives mechanistic insights that suggest a unique potential of low dose irreversible Btk inhibitors as atherothrombosis-focused antiplatelet drugs. Georg Thieme Verlag KG Stuttgart · New York.

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