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Cardiotoxicity of small-molecule kinase inhibitors in cancer therapy

Shuangli Zhu1, Kai Fu1, Sijia Li1

  • 1State Key Laboratory of Oncology in South China, Collaborative Innovation Center for Cancer Medicine, Guangdong Esophageal Cancer Institute, Guangdong Provincial Clinical Research Center for Cancer, Sun Yat-Sen University Cancer Center, Guangzhou, 510060, Guangdong, People's Republic of China.

Experimental Hematology & Oncology
|May 9, 2025
PubMed

Insights

Small-molecule kinase inhibitors (SMKIs) are effective cancer treatments but can cause cardiotoxicity. This review summarizes SMKI cardiotoxicity mechanisms and strategies for prevention and designing safer drugs.

Area of Science:

  • Oncology
  • Pharmacology
  • Cardiology

Background:

  • Small-molecule kinase inhibitors (SMKIs) represent a significant advancement in precision oncology, offering improved efficacy and reduced toxicity compared to traditional chemotherapy.
  • Despite their benefits, cardiotoxic adverse events associated with SMKIs are an emerging concern in cancer therapy.
  • The increasing clinical application of novel SMKIs necessitates a thorough understanding of their cardiac impact.

Purpose of the Study:

  • To comprehensively review the current understanding of cardiotoxicity induced by small-molecule kinase inhibitors (SMKIs) in cancer patients.
  • To discuss the latest findings on the mechanisms underlying SMKI-related cardiotoxicity.
  • To identify emerging strategies for preventing cardiotoxicity and designing next-generation targeted drugs with lower cardiac risk.

Main Methods:

  • Literature review of recent studies on small-molecule kinase inhibitors (SMKIs) and their cardiotoxicity.
  • Analysis of reported cardiotoxic adverse events in clinical trials and real-world data.
  • Synthesis of current knowledge on molecular and cellular mechanisms of SMKI cardiotoxicity.

Main Results:

  • Small-molecule kinase inhibitors (SMKIs) have shown significant efficacy in treating various cancers, with 89 approved since 2001.
  • Cardiotoxicity is a notable side effect of certain SMKIs, manifesting in variable degrees across different drugs and patient populations.
  • Emerging evidence points to specific molecular pathways and cellular targets involved in SMKI-induced cardiac dysfunction.

Conclusions:

  • Small-molecule kinase inhibitors (SMKIs) offer a valuable therapeutic strategy in oncology but require careful monitoring for cardiotoxicity.
  • Understanding the mechanisms of cardiotoxicity is crucial for developing effective prevention and management strategies.
  • Future research should focus on designing novel targeted therapies with reduced cardiac risk to improve long-term outcomes for cancer survivors.
Keywords:
CancerCardiotoxicitySmall-molecule kinase inhibitors

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