In summary, the present study demonstrated that the recombinant fusion protein Fv-LDP-D3 which consists of the Fv fragment of an anti-EGFR antibody, the apoprotein of lidamycin (LDP), and the third domain of human serum albumin (D3) and its pertinent drug conjugate (Fv-LDP-D3-AE) which is prepared by integrating the active enediyne chromophore (AE) into the fusion protein molecule both exhibited strong anti-tumor activity against EC cells in vitro and effectively inhibited the growth of cancer xenografts in vivo. This evidence concerns the gene EGFR and cancer.