PHASE-II STUDY OF DROLOXIFENE FOR TREATMENT OF METASTATIC COLORECTAL-CARCINOMA

Droloxifene (3-hydroxytamoxifen citrate) is a new synthetic non-steroidal antiestrogen which has been developed with high receptor binding affinity and possibly improved antiestrogenic activity in man. Recently, hormone receptors were observed in human colorectal carcinoma cell lines. For this reason, we treated 24 patients with advanced colorectal carcinoma and progressive disease with Droloxifen in a Phase-II trial. All patients exept three had been pretreated by cytotoxic chemotherapy. The dose of Droloxifene was 100 mg orally/day for at least eight weeks. Fifteen patients were evaluable for response. No complete or partial remission was observed. However, there were six patients (40%) showing tumor stabilization. The time to progression was twelve to 29 weeks. The toxicity of treatment was low and consisted of only few episodes of nausea, constipation and pain. The data suggest that Droloxifene has marginal activity for treatment of colorectal carcinoma.