Abstract: Anti-tumor therapy-related cardiotoxicity is the second leading cause of morbidity and mortality among cancer survivors after recurrent malignancy. The prevention of cardiovascular complications has become a great challenge in anti-tumor therapy. The pharmacokinetic-pharmacodynamic (PK-PD) model is a mathematical model-based approach to establishing the drug exposure-response relationship. The application of PK-PD model is highly beneficial for predicting cardiotoxicity of anti-tumor agents, so as to provide reference for cancer treatment strategies with high efficiency and low toxicity.