The invention provides a pharmaceutical composition for inhibiting proline-directed protein kinase FA/ glycogen synthase kinase 3α(PDPK FA/GSK-3α), experiments verified that the composition can be effectively inhibit PDPK FA/GSK-3α. In addition, through by inhibition of PDPK FA/GSK-3α can improve the clinical efficacy of cancer treatment and cure rate of.本發明提供一種醫藥組合物,用以抑制脯胺酸導引蛋白激酶FA/肝醣合成酶激酶3α,經實驗證實,此醫藥組合物可有效抑制脯胺酸導引蛋白激酶FA/肝醣合成酶激酶3α(PDPK FA/GSK-3α),此外,經過抑制脯胺酸導引蛋白激酶FA/肝醣合成酶激酶3α(PDPK FA/GSK-3α)可提高臨床上癌症的治療療效及治癒率。