The present invention relates to a ligand-cytotoxic drug conjugates, preparation method and pharmaceutical use thereof. More specifically, the present invention provides a general formula Pc-(X-Y-D)n of ligand-cytotoxic drug conjugates, their preparation method and their use in the preparation of a medicament for the treatment of cancer.本發明涉及配體-細胞毒性藥物偶聯物、其製備方法及其應用。具體而言,本發明提供了一種通式為Pc-(X-Y-D)n的配體-細胞毒性藥物偶聯物,其製備方法以及該配體-細胞毒性藥物偶聯物及含有其的醫藥組成物藉由受體調節在製備治療癌症的藥物中的用途。