Oral vitamin E supplementation has been reported to improve facial hyperpigmentation. α‐Tocopheryl ferulate (α‐TF) is a compound of α‐tocopherol (α‐T) and ferulic acid connected by an ester bond. Ferulic acid is also an antioxidant, and could scavenge free radicals induced by ultraviolet (UV) radiation, and thus maintain the long‐lasting antioxidative effect of α‐T. Previously we have reported that α‐TF inhibited melanogenesis in human melanoma cells. To know whether α‐TF might be useful as a whitening agent to improve and prevent facial hyperpigmentation, the depigmenting effect of α‐TF in normal human melanocytes was examined in this study. The results showed that 30 μg/ml of α‐TF dissolved in 150 μg/ml of lecithin inhibited melanization significantly without inhibiting cell growth. This phenotypic change was associated with the inhibition of tyrosinase and the degree of inhibition was dose dependent. No significant effect on DOPAchrome tautomerase (DT) activity was observed. These results suggest that α‐TF is a candidate for an efficient whitening agent which suppresses melanogenesis. In this paper, the role of α‐T and α‐TF in inhibiting biological reactions induced by reactive oxygen species (ROS) is also discussed.