Flutamide (SCH 13521) is an antiandrogen with about the same potency as cyproterone in rodent and canine species.

Androgen receptor:55 nM(Ki)

Flutamide使大鼠前列腺重量明显从319 mg降低到245 mg.联合使用Flutamide和黄体生成素释放激素激动剂引发副作用,使前列腺重量降低到101 mg,并且前列腺ODC活性明显下降.

Flutamide和亮丙瑞林联合使用可以用于治疗前列腺癌。Flutamide-OH是Flutamide的活性代谢物形式,直接结合大鼠垂体前叶雄性激素受体（Ki=55 nM）。Flutamide不影响小鼠乳腺癌Shionogi SC-l 15细胞在培养基中雄性激素敏感克隆的增殖,仅表现出抗雄激素作用,而没有雄激素作用。

Androgen Receptor Assay: Aliquots of 100 μl cytosol are incubated at 0-4°C for 18 h with 100 μl of the indicated saturating concentration of [3H]T in the presence or absence of increasing concentrations of nonlabeled T, DHT, flutamide (FLU) or flutamide-OH (FLU-OH). At the end of the incubation, free and bound T are separated by the addition of 200 μl dextran-coated charcoal (1 % charcoal, 0.1% dextran T-70, 0.1% gelatin, 1.5 mM EDTA and 50 mM Tris (pH 7.4)) for 15 min before centrifugation at 2300 × g for another 15 min at 0-4°C. Aliquots (350 μl) of the supernatant are transferred to scintillation vials with 10 ml of an aqueous counting solution before counting in a Beckman LS 330 counter.

Effect of flutamide on the growth of an androgen-sensitive clone (SEM-l) of mouse mammary carcinoma Shionogi cells in culture. The cells are incubated up to 40 days in medium (MEM + 2% dextran-coated charcoal extracted fetal calf serum) containing the compounds at a concentration of 1 μM. Media are changed every second day.(Only for Reference)