The invention belongs to the field of genetic engineering and biotechnology, and specifically discloses a design, preparation and pharmic application of a tumor-targeted TNF-related apoptosis-inducing ligands variant. The tumor-targeted TNF-related apoptosis-inducing ligands variant is generated by a fused protein which is consisted of the ligand of CD13, the connecting peptide and TNF-related apoptosis-inducing ligands variant, and which is by the construction of coding gene of the variant according to the technology of genetic engineering and clone, soluble recombinant expression and ordinary separation and purification. The variant, produced by the method of preparation of the tumor-targeted TNF-related apoptosis-inducing ligands variant, has favorable tumor-targeting characteristics and the significant enhancement of the anti-tumor effect. It is possible to reducing the required dosage of protein to the treatment effect, increasing the bioavailability, reducing the cost of treatment and overcome the potential toxic effects of the TNF-realated apoptosis-inducing ligand. Moreover, the preparation method of the tumor targeted TNF-related apoptosis-inducing ligands variant of the present invention provides a method for producing the variant of soluble expression and high concern of polymer forms and a process of separation and purification thereof.
