Abstract a-cypermethrin is one of the most potent insecticides used worldwide. This study was planned to evaluate the possible role of a-lipoic acid in a-cypermethrin induced toxicity in rats. The treated groups were; the control, α-cypermethrin, a-lipoic acid and a-cypermethrin, and a-lipoic acid groups. Our results showed that administration of a-cypermethrin caused a significant decrease in RBC count, PCV, and Hb content and an increase in WBC count. Also, a- cypermethrin caused a significant increase in the levels of cholesterol, TGs, LDL-Cand VLDL-C, while the HDL-C was decreased. Also, a-cypermethrin caused a reduction in serum testosterone, FSH, and LH levels in intoxicated rats. Furthermore, the co-administration of a-lipoic acid mitigated the toxicity of a-cypermethrin by partially normalizing these biochemical parameters. Our results were supported by histopathological observations of the testis. Our data suggest that a-lipoic acid may have a protective role against a-cypermethrin induced toxicity in rats.