The present invention relates to a skin whitening composition prepared with imatinib and the application thereof. The composition comprises imatinib, alcohols, nut oils, polysaccharide complex, esters, and pharmaceutically acceptable carrier, excipient, thinner, and adjuvant. The composition uses the approach of reducing melanin content in cells through inhibiting tyrosinase activity to achieve the efficacy of skin whitening.本發明係為一種使用伊馬替尼(imatinib)製備用於皮膚美白之組合物及其用途,其中該組合物係包括:伊馬替尼、醇類、堅果油、複合多醣體、酯類,及藥學上可接受之載劑、賦形劑、稀釋劑、輔劑等;且該組合物係以透過抑制酪胺酸酶活性來減少細胞內黑色素含量的方式,來達到美白之功效。