Compositions and methods are provided that are effective in treating skin hyperproliferative disorders. These include a topical pharmaceutical preparation that includes a compound that has two or more of a SRC-kinase inhibiting activity, a tubulin polymerization inhibiting activity, an activity that arrests the cell cycle at G2/M, and an activity that induces apoptosis. The compound KX01 is provided as an example of such a compound. The topical pharmaceutical preparation further includes a vitamin D derivative or a retinoid, where the combination provides a synergistic effect. Use of the topical pharmaceutical preparation can be combined with exposure to blue, UVA, or UVB light, which provides a synergistic effect.本發明提供了能有效治療皮膚過度增生性疾病的組合物及方法。前述組合物及方法包括局部施用的醫藥製劑,其包括一化合物,前述化合物具有一活性,前述活性包括抑制SRC-激酶、抑制微管蛋白聚合作用、G2/M細胞週期停滯及誘導細胞凋亡所組成的群組中的兩種或以上。前述化合物的實例為KX01。局部醫藥製劑更包括維生素D衍生物或類視色素(retinoid),其中前述組合提供協同作用。局部施用的醫藥製劑可以與暴露於藍色、UVA或UVB光來組合使用,以提供協同作用。