Akimoto S
Department of Urology, Inoue Memorial Hospital.
Nihon Rinsho. 1998 Aug;56(8):2135-9.
The antiandrogen withdrawal syndrome was first reported in patients with prostate cancer who manifested disease progression after total androgen blockage therapy with medical or surgical castration and pure antiandrogen, flutamide; discontinuation of flutamide resulted in a decline in prostate specific antigen and, in some cases, with clinical response. Same phenomena have been reported after the withdrawal of casodex, chlormadinone acetate, megestrol acetate, diethylstilbestrol, and estramustine phosphate. Mutations in the androgen receptor(AR) gene were discovered in clinical specimens of human prostate cancer patients who showed this syndrome and some of these being identical to the mutation found in LNCaP prostate cancer cell line. Another mechanism otherwise the point mutation of AR would be also speculated.
抗雄激素撤药综合征最初在前列腺癌患者中被报道，这些患者在接受药物或手术去势及单纯抗雄激素药物氟他胺进行全雄激素阻断治疗后出现疾病进展；停用氟他胺导致前列腺特异性抗原下降，在某些情况下还伴有临床反应。在停用比卡鲁胺、醋酸氯地孕酮、醋酸甲地孕酮、己烯雌酚和磷酸雌莫司汀后也报道了相同现象。在出现该综合征的人类前列腺癌患者的临床标本中发现了雄激素受体（AR）基因突变，其中一些与LNCaP前列腺癌细胞系中发现的突变相同。另外也推测存在AR点突变的其他机制。
