Ibrutinib-Associated Cardiotoxicity: From the Pharmaceutical to the Clinical

Drug Des Devel Ther. 2022 Sep 20:16:3225-3239. doi: 10.2147/DDDT.S377697. eCollection 2022.

Abstract

Ibrutinib is the first-in-class Bruton tyrosine kinase (BTK) inhibitor that has revolutionized the treatment of B cell malignancies. Unfortunately, increased incidences of cardiotoxicity have limited its use. Despite over a decade of research, the biological mechanisms underlying ibrutinib cardiotoxicity remain unclear. In this review, we discuss the pharmacological properties of ibrutinib, the incidence and mechanisms of ibrutinib-induced cardiotoxicity, and practical management to prevent and treat this condition. We also synopsize and discuss the cardiovascular adverse effects related to other more selective BTK inhibitors, which may guide the selection of appropriate BTK inhibitors.

Keywords: BTK inhibitors; atrial fibrillation; cardio-oncology; cardiotoxicity; ibrutinib.

Publication types

  • Review

MeSH terms

  • Adenine* / analogs & derivatives
  • Agammaglobulinaemia Tyrosine Kinase* / antagonists & inhibitors
  • Cardiotoxicity* / etiology
  • Humans
  • Leukemia, Lymphocytic, Chronic, B-Cell* / drug therapy
  • Piperidines* / adverse effects
  • Piperidines* / therapeutic use
  • Protein Kinase Inhibitors* / adverse effects
  • Protein Kinase Inhibitors* / therapeutic use

Substances

  • Piperidines
  • Protein Kinase Inhibitors
  • ibrutinib
  • Agammaglobulinaemia Tyrosine Kinase
  • Adenine