The present invention discloses uses of the human ZFX gene and drugs associated therewith. Also disclosed are uses of the human ZFX gene in tumor treatment, tumor diagnosis, and drug preparation. Further disclosed are small interfering RNA (siRNA), and nucleic acid and lentivirus encoding the siRNA to the human ZFX gene and uses thereof. The siRNA and nucleic acid and lentivirus encoding the siRNA provided by the present invention can specifically inhibit the expression of human ZFX gene. Lentiviruses in particular can efficiently infect target cells, inhibit ZFX expression in target cells, and inhibit the growth of tumor cells, thus promote tumor apoptosis and have great significance in tumor treatment.