产地国家：美国 处方药：是 所属类别： 500毫克/片 60片/瓶 包装规格： 500毫克/片 60片/瓶 计价单位：瓶 生产厂家英文名：JOM PHARMACEUTICAL 原产地英文商品名：ZYTIGA Filmtabl 500mg  60Stk 原产地英文药品名：abiraterone acetate 中文参考商品译名：ZYTIGA薄膜包衣片 500毫克/片 60片/瓶 中文参考药品译名：醋酸阿比特龙

简介：

近日，美国食品药品管理局(FDA)批准了每日1次口服药物Zytiga(醋酸阿比特龙)的扩大适应证申请。此前，Zytiga仅被批准联合泼尼松用于曾接受含多烯紫杉醇化疗的转移性去势难治性前列腺癌(mCRPC)患者。基于这项新批准令，现在Zytiga联合泼尼松可更早用于mCRPC连续治疗，即在化疗之前使用。 作用机理：醋酸阿比特龙（ZYTIGA）在体内转化到阿比特龙，雄激素生物合成抑制剂，抑制17α羟化酶/ C17,20裂解酶（CYP17）。这种酶在睾丸，肾上腺和前列腺肿瘤组织中表达的和所需的雄激素合成。CYP17催化两个连续反应：1）孕烯醇酮，孕激素到其17α羟基衍生物由17α羟化酶活性分别转换和2）随后形成的脱氢表雄酮（DHEA）和雄烯二酮，由C17，20裂解酶活性DHEA和雄甾烯二酮是雄激素和可通过阿比特龙也可以导致增加的盐皮质生产由肾上腺CYP17的睾丸激素。抑制的前体[见警告和注意事项]。雄激素敏感的前列腺癌响应治疗其降低雄激素水平。雄激素剥夺疗法，如用GnRH激动剂或睾丸切除术治疗，减少雄激素产生在睾丸，但不通过肾上腺或肿瘤影响雄激素的产生。ZYTIGA在患者在安慰剂对照的3期临床试验降低血清睾酮等雄激素，它不是必要监测ZYTIGA对血清睾酮水平的影响。在血清前列腺特异性抗原（PSA）水平的变化，可以观察到，但没有示出在个体患者的临床益处相关。 适应症和用法：ZYTIGA是结合泼尼松患有转移性去势抗性前列腺癌的治疗指示的CYP17抑制剂。 用法用量：推荐剂量：ZYTIGA 1000毫克组合每日口服施用一次与强的松5毫克（2个500毫克片剂或四个250毫克的片剂）口服给药每天两次ZYTIGA必须空腹采取否应该进食至少两ZYTIGA剂量前小时取出并ZYTIGA的剂量服用后至少一个小时。片剂应先用清水整个吞下。不压碎或咀嚼药片。患者的基线中度肝损伤（Child-Pugh分级B级），每天一次减少ZYTIGA起始剂量至250mg。对于谁在治疗过程中发展的肝毒性的患者，持有ZYTIGA直至痊愈。再治疗可以减少剂量开始。如果出现严重的肝毒性ZYTIGA应停药。 剂型和规格：薄膜包衣片：500毫克薄膜包衣片：250毫克未包衣片剂：250毫克 禁忌症：怀孕。 警告和注意事项：盐皮质激素过多使用：用ZYTIGA患者慎用心血管疾病ZYTIGA患者到IV心脏的安全性与左室射血分数<50％或NYHA III或IV级心脏衰竭研究1或左室射血分数<50％或NYHA分级II的历史在研究2故障是不成立的。对照治疗前高血压和正确低钾血症。监测血压，血清钾和症状体液潴留的至少每月一次。肾上腺皮质功能减退：监测症状和糖皮质激素的肾上腺皮质功能减退剂量增加的迹象可能在和紧张的情况后表示之前。肝毒性:可能是严重的和致命监测肝功能和修改，中断或终止ZYTIGA剂量的建议。 不良反应：最常见的不良反应（≥10％）是疲劳，关节肿胀或不适，水肿，潮热，腹泻，呕吐，咳嗽，高血压，呼吸困难，尿路感染和挫伤。最常见的实验室异常（> 20％）是贫血，碱性磷酸酶升高，高甘油三酯血症，淋巴细胞减少，高胆固醇血症，高血糖症，升高的AST，低磷血症，ALT升高和低钾血症。 药物相互作用：CYP3A4诱导:. ZYTIGA治疗期间避免强CYP3A4诱导如果CYP3A4强诱导剂必须同时给予，增加ZYTIGA给药频率。CYP2D6的底物:避免ZYTIGA的共同施用与具有窄的治疗指数如果替代的治疗不能使用，谨慎操作并考虑伴随CYP2D6基板的剂量减少CYP2D6的底物。 特殊人群中使用：不要在患者的基线严重肝受损（Child-Pugh类别C）使用ZYTIGA。

英文版说明书：

ZYTIGATM(abiraterone acetate) in combination with prednisone is indicated for the treatment of patients with metastatic castration-resistant prostate cancer (CRPC) who have received prior chemotherapy containing docetaxel.IMPORTANT SAFETY INFORMATIONContraindicationsZYTIGATM may cause fetal harm (Pregnancy Category X) and is contraindicated in women who are or may become pregnant.Warnings and PrecautionsHypertension, Hypokalemia and Fluid Retention Due to Mineralocorticoid ExcessMineralocorticoid Excess - Use with caution in patients with a history of cardiovascular disease or with medical conditions that might be compromised by increases in hypertension, hypokalemia and fluid retention.Safety has not been established in patients with LVEF < 50% or NYHA Class III or IV heart failure. Control hypertension and correct hypokalemia before and during treatment.Monitor blood pressure, serum potassium, and symptoms of fluid retention at least monthly.Adrenocortical InsufficiencyAdrenocortical Insufficiency (AI) has been reported in clinical trials after an interruption of daily steroids and/or with concurrent infection or stress. Use caution and monitor for symptoms and signs of AI if prednisone is stopped or withdrawn or if the patient experiences unusual stress. Perform appropriate tests, if indicated, to confirm AI.Increased dosages of corticosteroids may be used before, during and after stressful situations.HepatotoxicityHepatotoxicity - Increases in liver enzymes have led to drug interruption, dose modification and/or discontinuation. Monitor liver function and modify, withhold or discontinue ZYTIGATM dosing as recommended (See Prescribing Information for more information).Food EffectFood Effect - ZYTIGATM must be taken on an empty stomach. Exposure of abiraterone increases up to 10-fold when abiraterone acetate is taken with meals.No food should be eaten for at least two hours before the dose of ZYTIGATM is taken and for at least one hour after the dose of ZYTIGATM is taken.Adverse ReactionsThe most common adverse reactions (≥ 5%) reported in clinical trials were joint swelling or discomfort, hypokalemia, edema, muscle discomfort, hot flush, diarrhea, urinary tract infection, cough, hypertension, arrhythmia, urinary frequency, nocturia, dyspepsia and upper respiratory tract infection.Drug InteractionsZYTIGATM is an inhibitor of the hepatic drug-metabolizing enzyme CYP2D6. Avoid co-administration with CYP2D6 substrates that have a narrow therapeutic index.If an alternative cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.Additionally, abiraterone is a substrate of CYP3A4