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Flutamide

氟他胺

Mechanism of action:

Flutamide 是一種醯替苯胺（anilide）衍生物。Flutamide 及其主要活性代謝物 hydroxyflutamide 會與雄激素受體（androgen receptor）結合，阻止睪酮（testosterone）以及二氫睪酮（dihydrotestosterone）與受體結合，使前列腺癌細胞中的生長與存活相關的基因表達量降低。

​Reference(s):

1. Chang HC et al. (1999). Suppression of Delta(5)-androstenediol-induced androgen receptor transactivation by selective steroids in human prostate cancer cells. Proc Natl Acad Sci U S A. 


2. Martelli A et al. (2000). Evaluation of flutamide genotoxicity in rats and in primary human hepatocytes. Pharmacol Toxicol. 


3. Montalvo L et al. (2000). Effect of flutamide-induced androgen-receptor blockade on adenylate cyclase activation through G-protein coupled receptors in rat prostate. Cell Signal.

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