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-L-Dr of ligand - cytotoxic drug conjugate, preparation thereof, and the use of the ligand - cytotoxic drug conjugate thereof and a pharmaceutical composition thereof as a medicament by receptor modulating for the treatment of cancer, wherein definitions of substituent groups in formula (I) are the same as definitions in the specifications.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-L-Dr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藥物組成物藉由受體調節在製備治療癌症的藥物中的用途,其中通式(PC-L-Dr)中的各取代基與說明書中的定義相同。