In a comparative pharmakokinetic analysis between tamoxifen (T) and th
e new antiestrogen droloxifene (D), 28 patients with metastatic breast
cancer have been treated since 1985 with 40 mg per os daily of the an
tiestrogens in a double-blind randomised study. During the first 3 tre
atment months and following the end of treatment, blood samples were t
aken at well-defined times in order to investigate routine laboratory
parameters as well as serum concentrations of T and D and their metabo
lites. Due to its completely different metabolism pathway, the pharmak
okinetic data of droloxifene in serum show quick absorption, almost no
accumulation and rapid elimination. This enables the substance to rea
ct sooner with its target, resulting in shorter times to treatment eff
ects compared with tamoxifen. Finally the therapeutic flexibility will
be improved.