XTANDI 適用於治療患有去勢抵抗性前列腺癌 (CRPC)、轉移性去勢敏感性前列腺癌 (mCSPC) 和非轉移性去勢敏感性前列腺癌 (nmCSPC) 並伴有高風險生化復發 (high-risk BCR) 的患者。
XTANDI is indicated for the treatment of patients with castration-resistant prostate cancer (CRPC), metastatic castration-sensitive prostate cancer (mCSPC), and non-metastatic castration-sensitive prostate cancer (nmCSPC) with high-risk biochemical recurrence (high-risk BCR).
Enzalutamide 是一種雄激素受體抑制劑，作用於雄激素受體信號通路的不同步驟。Enzalutamide 通過競爭性抑制雄激素與雄激素受體的結合，從而抑制雄激素受體的核轉位及其與 DNA 的相互作用。其主要代謝物 N-desmethyl enzalutamide 在體外表現出與 enzalutamide 相似的活性。Enzalutamide 在體外能減少前列腺癌細胞的增殖並誘導其死亡，並在小鼠前列腺癌異種移植模型中減少腫瘤體積。
Enzalutamide is an androgen receptor inhibitor that acts on different steps in the androgen receptor signaling pathway. Enzalutamide has been shown to competitively inhibit androgen binding to androgen receptors; consequently, it inhibits nuclear translocation of androgen receptors and their interaction with DNA. A major metabolite, N-desmethyl enzalutamide, exhibited similar in vitro activity to enzalutamide. Enzalutamide decreased proliferation and induced cell death of prostate cancer cells in vitro, and decreased tumor volume in a mouse prostate cancer xenograft model.
Enzalutamide 在第28天達到穩態，其AUC約為單劑量的8.3倍。穩態下，enzalutamide 和 N-desmethyl enzalutamide 的平均最大濃度（Cmax）分別為 16.6 g/mL（23%）和 12.7 g/mL（30%），平均最低濃度（Cmin）分別為 11.4 g/mL（26%）和 13.0 g/mL（30%）。Enzalutamide 在日劑量範圍30 mg至360 mg內顯示出近似的藥代動力學特性。
Enzalutamide achieves steady-state by Day 28 and its AUC accumulates approximately 8.3-fold relative to a single dose. At steady-state, the mean (%CV) maximum concentration (Cmax) for enzalutamide and N-desmethyl enzalutamide are 16.6 g/mL (23%) and 12.7 g/mL (30%), respectively, and the mean (%CV) minimum concentrations (Cmin) are 11.4 g/mL (26%) and 13.0 g/mL (30%), respectively. Enzalutamide showed approximately dose-proportional pharmacokinetics over the daily dose range of 30 mg to 360 mg.
無。
None.
XTANDI 在女性中的安全性和有效性尚未確立。根據動物研究和作用機制，XTANDI 可導致胎兒傷害和妊娠喪失。在懷孕小鼠的生殖毒性研究中，口服給予 enzalutamide 導致胚胎-胎兒毒性，包括胚胎-胎兒致死性、、裂和缺失顎骨。
The safety and efficacy of XTANDI have not been established in females. Based on animal reproductive studies and its mechanism of action, XTANDI can cause fetal harm and loss of pregnancy. In animal reproductive toxicity studies, oral administration of enzalutamide to pregnant mice caused embryo-fetal toxicity, including embryo-fetal lethality, cleft palate, and absent palatine bone.
XTANDI 在女性中的安全性和有效性尚未確立。尚無有關 XTANDI 是否存在於人乳中的資料，也不清楚其對哺乳嬰兒的影響或對乳汁產生的影響。在泌乳大鼠中，給予單次口服 enzalutamide 後，其代謝物在乳汁中的濃度高於血漿。
The safety and efficacy of XTANDI have not been established in females. There is no information available on the presence of XTANDI in human milk, the effects on the breastfed infant, or the effects on milk production. In lactating rats, enzalutamide and its metabolites were present in milk at concentrations higher than in plasma following a single oral administration.
常見副作用包括無力狀態、頭暈、高血壓、熱潮紅、噁心和便秘。嚴重副作用包括癲癇發作、後部可逆性腦病綜合症（PRES）、過敏反應、缺血性心臟病、跌倒和骨折。
Common adverse reactions include asthenic conditions, dizziness, hypertension, hot flush, nausea, and constipation. Serious adverse reactions include seizure, posterior reversible encephalopathy syndrome (PRES), hypersensitivity, ischemic heart disease, falls, and fractures.
XTANDI 的推薦劑量為每日口服160 mg，可與食物同服或不同服。吞服膠囊或片劑，不要咀嚼、溶解或打開膠囊，也不要切割、壓碎或咀嚼片劑。
The recommended dosage of XTANDI is 160 mg administered orally once daily with or without food. Swallow capsules or tablets whole. Do not chew, dissolve, or open the capsules. Do not cut, crush, or chew the tablets.
XTANDI 在兒童中的安全性和有效性尚未確立。
The safety and efficacy of XTANDI in pediatric patients have not been established.
根據資料，對於輕度至中度腎功能不全（CLcr 30 mL/min）患者，XTANDI 的藥代動力學無臨床顯著差異。重度腎功能不全和終末期腎病（CLcr < 30 mL/min）的患者尚未進行研究。
No clinically meaningful differences in the pharmacokinetics of XTANDI were observed in patients with mild to moderate renal impairment (CLcr 30 mL/min). XTANDI has not been studied in patients with severe renal impairment and end-stage renal disease (CLcr < 30 mL/min).
根據資料，對於輕度至中度肝功能不全（Child-Pugh A, B）患者，XTANDI 的藥代動力學無臨床顯著差異。重度肝功能不全（Child-Pugh C）的患者應慎用。
No clinically meaningful differences in the pharmacokinetics of XTANDI were observed in patients with mild to moderate hepatic impairment (Child-Pugh A, B). XTANDI should be used with caution in patients with severe hepatic impairment (Child-Pugh C).