Abstract: Compared with traditional chemotherapy, targeted cancer therapy is a novel strategy that inhibits the key molecules in signalling pathways involved in carcinogenesis and tumor metastasis. Tyrosine kinase inhibitors (TKIs) are multi-targeted anti-cancer agents for the treatment of renal cell carcinoma, gastrointestinal stromal tumor and pancreatic cancer, and can exert targeted inhibition on oncogene-associated receptor tyrosine kinase (RTK). Interestingly, besides death related to the malignancy itself, chemotherapy-related adverse cardiovascular events are the leading cause of death in cancer patients. In this review, we focused on several small-molecule TKIs(sunitinib, sorafenib, pazopanib, axitinib) and the incidence of cardiotoxicities associated with their use, including left ventricular dysfunction, ischemic cardiomyopathy, hypertension and thromboembolic events, and summarized the potential molecular mechanisms of their adverse cardiovascular effects.