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Bicalutamide

比卡魯胺

Mechanism of action:

Bicalutamide 是一種非類固醇型雄激素受體拮抗劑（non-steroidal anti-androgen）。在正常情況下，睪酮（testosterone）與其代謝物二氫睪酮（DHT，dihydrotestosterone）會與雄激素受體（androgen receptor）結合，形成複合體，進入細胞核活化雄激素反應基因（androgen-responsive genes），促進前列腺細胞增生與存活。Bicalutamide 會競爭性拮抗雄激素受體，而無法形成該複合體進入細胞核，導致雄激素反應基因的轉錄活性下降，細胞增殖相關訊號受抑，並可影響細胞存活與凋亡路徑。

​Reference(s):

1. Wang LG et al. (1998). Androgen antagonistic effect of estramustine phosphate (EMP) metabolites on wild-type and mutated androgen receptor. Biochem Pharmacol. 


2. 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 USA.

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