The effects of triptorelin (Decapeptyl®) and heparin, alone or in combination, on the intracellular concentration of estradiol (E2) after incubation of estrone sulfate (E1S) with the MCF-7 mammary cancer cells was investigated. Although heparin (10 mg/l culture medium) or Decapeptyl® (5×10−7 or 5 × 10−5mol/l) did not affect the levels of radioactive E2 after incubation with [3H]E1S, the combination of Decapeptyl® and heparin significantly decreased the radioactive uptake and the intracellular concentrations of [3H]E2. In the absence of Decapeptyl® and heparin incubations with E1S, the resulting E2 concentration (in nmol/kg DNA±sd) was 558±44; after heparin (10 mg/l) plus Decapeptyl® (5× 10−7 or 5× 10−5 mol/l) the values were 389±55 and 165±18, respectively. It is concluded that Decapeptyl® with heparin can decrease very significantly the conversion of E1S to E2 in MCF-7 cells, an observation that suggests new possibilities for the control of E2 in hormone-dependent breast cancer.