Suramin at 100 to 800 micrograms/ml caused a dose dependent growth inhibition in three (Zr-75-1, BT 549 and HS-578T) parental human breast cancer cell lines and their corresponding sublines with acquired doxorubicin (dox) and multi-drug resistance. The effect was significantly more marked after 7 days suramin exposure compared with 3 days. The oestrogen and progesterone receptor rich cell line Zr-75-1 was more responsive to suramin compared with the other two lines. The sublines Zr-75-1-dox and HS-578T-dox with an increased expression of the permeability glycoprotein (P-gp) demonstrated a significantly decreased cell survival compared with corresponding parental cell lines at 3 and 7 days exposure of suramin, respectively. The subline BT 549-dox with multi-drug resistance without P-gp expression had a significantly impaired response after 3 days suramin compared with the parental line. These results indicate that suramin may be a potential therapeutic agent for the breast cancer patients with P-gp expression and multi-drug resistance.