Provide ligand-cytotoxic drug conjugate that a kind of general formula (I) is PC-L-Dr, preparation method and the ligand-cytotoxic drug conjugate and the purposes containing its pharmaceutical composition by regulation in the drug of preparation treating cancer.提供了一種通式(Ⅰ)爲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合物通過受體調節在製備治療癌症的藥物中的用途。