This study aims to determine the toxicity, genotoxicity and antioxidative defense capacities of isopentanyl ferulate (IF), an ester derivative of ferulic acid (FA). Therefore, albino mice (25-30 g) were treated with 1000 to 3000 mg/kg orally (p.o.) and intraperitoneally (i.p.) to determine median lethal dose (LD 50), biochemical and hematological parameters, motor coordination and genotoxic activity by comet assay. In addition, oxidative defense was assessed in Saccharomyces cerevisiae with one proficient (Sod wt), three single mutant (Sod1∆, Sod2∆ and Cat1∆) and two double mutants (Sod1∆Sod2∆ and Sod1∆Cat1∆), where IF in a dose range of 0.10 to 0.30 g/ml was used. Results suggest that IF produced LD 50 by 1494.54 mg/kg. There was a bit change in biochemical and hematological parameters compared to the control group. Although, IF did not affect locomotor activity in test animals (both sexes) assessed by open field test (OFT) but it produced genotoxic activity at doses 1500 mg/kg (i.p.) and 3000 mg/kg (p.o.), whosever is higher than the LD 50. Antioxidative defense to the S. cerevisiae cells and damage repair capability in both comet and S. cerevisiae assays indicate IF for a promising pharmacological moiety. In conclusion, IF produced low toxicity, genotoxicity at high dose with antioxidative defense and damage repair capability.