The study was purposed to investigate the synergistic reversal effect of Chinese medicine compound FFJZ in combination with cyclosporine A (CsA) on the multidrug resistance (MDR) of human leukemia K562/VCR cell line, as to search effective combination of MDR modulators. MTT (methyl-thazol-tetrazolinum) assay were used to determine the cytotoic and reversal effects on K562/VCR cell line, FCM (flow cytometry) was used to assess the intracellular adriamycin (ADM) concentration and the expression of P-gp in cells. The results showed that the FFJZ in combination with CsA could reverse the drug-resistance of K562/VCR cells and increase the sensitivity K562/VCR cells to adriamycin. They had not the toxic effect on the K562/VCR cells in effective dose and no significant influence on P-gp positive rate of the K562/VCR cells. It is concluded that the FFJZ in combination with CsA may become a safe and effective multidrug resistance-reversing agent with low toxicity in leukemia chemotherapy.