Abstract: Anthracyclines have attracted growing attention because of their significant anti-cancer effect, safe clinical application, and great market demand. However, the cardiac toxicity of anthracycline limits its dosage. Dexrazoxane is the only approved cardioprotective agent that has been widely accepted. Dexrazoxane has also been recommended by many guidelines in China and overseas, such as the American Society of Clinical Oncology 2008 Clinical Practice Guideline. However, controversy surrounds the details of the clinical use of Dexrazoxane. In this paper, we have discussed the possibility that Dexrazoxane influences anti-tumor efficacy. In addition, we have tackled the administration, safety, and other possible cardioprotective effects of Dexrazoxane.