Objective: To evaluate the cardioprotective effects of ketotifen and to assess its activity as an iron-chelating agent in patients receiving anthracyclines for the treatment of breast cancer. Method: The study was a randomized prospective controlled trial. 111 Eligible patients were recruited for the study and divided into two groups; a control group of 55 patients received their standard anthracycline chemotherapy; a ketotifen group of 56 patients received their standard anthracycline plus ketotifen. Ketotifen was given orally 1 mg three times daily for six consecutive cycles of treatment. The echocardiogram for each patient was recorded two times at the baseline and at the end of treatment. As well, blood samples were collected for all the patients. Results: The findings showed a statistically significant reduction in the mean serum levels of common cardiotoxicity accompanied biomarkers in the ketotifen group compared with the control group (P ≤ 0.05). Whereas, mean levels of total iron binding capacity was significantly elevated in the ketotifen group (P ≤ 0.001). There was a direct correlation between the level of iron and the LDH (r = + 0.79). On the other hand, there were indirect correlations between the LDH level and both of the percentage of ejection fraction and the total iron binding capacity (r = - 0.69 and -0.697 respectively). Conclusion: Oral administration of ketotifen appears to be efficient and safe as a novel cardio-protective agent for prevention of anthracyclines induced cardiotoxicity. Additionally, ketotifen suggested showing a beneficial effect in iron overload inducing diseases such as COVID-19.