Ibrutinib promotes atrial fibrillation by inducing structural remodeling and calcium dysregulation in the atrium

Heart Rhythm. 2019 Sep;16(9):1374-1382. doi: 10.1016/j.hrthm.2019.04.008. Epub 2019 Apr 5.

Abstract

Background: Ibrutinib is a novel antitumor drug that targets Bruton tyrosine kinase for treatment of chronic lymphocytic leukemia. Atrial fibrillation (AF) occurs in 5%-9% of patients during treatment, but the underlying mechanisms remain unclear.

Objective: The purpose of this study was to develop a mouse model of ibrutinib-induced AF and investigate its proarrhythmic mechanisms.

Methods: In C57BI/6 mice in the ibrutinib and control groups, ibrutinib (25 mg/kg/d) or vehicle (hydroxypropy1-β-cyclodextrin), respectively, was administered orally for 4 weeks. Transesophageal burst stimulation then was used to induced AF. To evaluate the underlying mechanism of AF, cardiac echocardiography was performed. Ca2+ handling and action potentials in atrial myocytes were evaluated.

Results: Compared with the control group, the ibrutinib group showed (1) a higher incidence and longer duration of AF with transesophageal burst stimulation; (2) increased left atrial mass, as indicated by echocardiography; (3) significant myocardial fibrosis in the left atrium on Masson trichrome staining; (4) Ca2+ handling disorders in atrial myocytes, such as reduced Ca2+ transient amplitude, enhanced spontaneous Ca2+ release, and reduced sarcoplasmic Ca2+ capacity; (5) enhanced delayed afterdepolarization in atrial myocytes; and (6) increased CaMKII expression and phosphorylation of RyR2-Ser2814 and PLN-Thr17.

Conclusion: The present study established a mouse model of AF by oral administration of ibrutinib for 4 weeks. The arrhythmogenic mechanisms underlying this model likely are associated with structural remodeling and Ca2+ handling disorders in the atrium.

Keywords: Atrial fibrillation; Atrial fibrosis; Calcium/calmodulin-dependent protein kinase II; Ibrutinib; Structural remodeling.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenine / analogs & derivatives
  • Agammaglobulinaemia Tyrosine Kinase / antagonists & inhibitors*
  • Animals
  • Antineoplastic Agents / pharmacology
  • Atrial Fibrillation* / etiology
  • Atrial Fibrillation* / metabolism
  • Atrial Fibrillation* / physiopathology
  • Atrial Remodeling / drug effects*
  • Calcium / metabolism*
  • Calcium Signaling / drug effects*
  • Disease Models, Animal
  • Echocardiography / methods
  • Heart Atria* / diagnostic imaging
  • Heart Atria* / drug effects
  • Heart Atria* / pathology
  • Heart Atria* / physiopathology
  • Leukemia, Lymphocytic, Chronic, B-Cell / drug therapy
  • Mice
  • Myocytes, Cardiac / drug effects
  • Myocytes, Cardiac / metabolism
  • Piperidines
  • Pyrazoles / pharmacology*
  • Pyrimidines / pharmacology*

Substances

  • Antineoplastic Agents
  • Piperidines
  • Pyrazoles
  • Pyrimidines
  • ibrutinib
  • Agammaglobulinaemia Tyrosine Kinase
  • Adenine
  • Calcium