Endothelium as a Source of Cardiovascular Toxicity From Antitumor Kinase Inhibitors

Arterioscler Thromb Vasc Biol. 2024 Oct;44(10):2143-2153. doi: 10.1161/ATVBAHA.124.319864. Epub 2024 Aug 15.

Abstract

Kinase inhibitors (KIs) targeting oncogenic molecular pathways have revolutionized cancer therapy. By directly targeting specific tumor-driving kinases, targeted therapies have fewer side effects compared with chemotherapy. Despite the enhanced specificity, cardiovascular side effects have emerged with many targeted cancer therapies that limit long-term outcomes in patients with cancer. Endothelial cells lining all blood vessels are critical to cardiovascular health and are also exposed to circulating levels of systemic anticancer therapies. Both on- and off-target perturbation of signaling pathways from KIs can cause endothelial dysfunction, resulting in cardiovascular toxicity. As such, the endothelium is a potential source, and also a therapeutic target for prevention, of cardiovascular toxicity. In this review, we examine the evidence for KI-induced endothelial cell dysfunction as a mechanism for the cardiovascular toxicities of vascular endothelial growth factor inhibitors, BCR-Abl (breakpoint cluster region-Abelson proto-oncogene) KIs, Bruton tyrosine inhibitors, and emerging information regarding endothelial toxicity of newer classes of KIs.

Keywords: cardio-oncology; cardiotoxicity; endothelium; receptors, vascular endothelial growth factor; tyrosine kinase inhibitors.

Publication types

  • Review
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents* / adverse effects
  • Antineoplastic Agents* / toxicity
  • Cardiotoxicity
  • Cardiovascular Diseases* / chemically induced
  • Endothelial Cells / drug effects
  • Endothelial Cells / enzymology
  • Endothelial Cells / metabolism
  • Endothelial Cells / pathology
  • Endothelium, Vascular / drug effects
  • Endothelium, Vascular / enzymology
  • Endothelium, Vascular / metabolism
  • Endothelium, Vascular / pathology
  • Endothelium, Vascular / physiopathology
  • Humans
  • Neoplasms / drug therapy
  • Protein Kinase Inhibitors* / adverse effects
  • Proto-Oncogene Mas*
  • Signal Transduction / drug effects
  • Vascular Endothelial Growth Factor A / antagonists & inhibitors
  • Vascular Endothelial Growth Factor A / metabolism

Substances

  • Protein Kinase Inhibitors
  • Proto-Oncogene Mas
  • MAS1 protein, human
  • Antineoplastic Agents
  • Vascular Endothelial Growth Factor A