近日，美国食品和药物管理局（FDA）批准新型抗癌口服片剂Nubeqa（darolutamide 中文译名：达洛鲁胺 ）口服片剂上市，用于非转移性去势抵抗性前列腺癌（nmCRPC）患者的治疗。Nubeqa是一种口服非甾体雄激素受体（AR）抑制剂，具有独特的化学结构，以高亲和力结合受体，表现出强烈的拮抗活性，从而抑制受体功能和前列腺癌细胞的生长。
批准日期：2019年7月31日 公司：拜耳公司
NUBEQA（达洛鲁胺 [darolutamide]）片剂，口服使用
美国最初批准：2019年
作用机制
Darolutamide是雄激素受体（AR）抑制剂。Darolutamide竞争性抑制雄激素结合，AR核转位和AR介导的转录。主要代谢产物酮-达洛他定表现出相似的体外活性todarolutamide。此外，darolutamide在体外作为孕酮受体（PR）拮抗剂起作用（与AR相比，活性约为1％）。在前列腺癌的小鼠异种移植模型中，Darolutamide降低体外前列腺癌细胞增殖和肿瘤体积。
适应症和用法
NUBEQA是一种雄激素受体抑制剂，适用于治疗非转移性去势抵抗性前列腺癌患者。
剂量和给药
NUBEQA 600毫克（两片300毫克片剂）每日口服两次。
燕子片整个。拿NUBEQA食物。
患者还应同时接受促性腺激素释放激素（GnRH）类似物或应进行双侧睾丸切除术。
剂量形式和强度
片剂：300mg
禁忌症
没有。
警告和注意事项
胚胎 - 胎儿毒性：NUBEQA会导致胎儿受伤和失去怀孕。向具有生殖潜力的女性伴侣的男性提供建议，以使用有效的避孕措施。
不良反应
最常见的不良反应（≥2％）是疲劳，四肢疼痛和痉挛。
要报告可疑的不良反应，请致电1-888-842-2937联系拜耳，或致电1-800-FDA-1088或WWW.FDA.GOV/MEDWATCH联系FDA。
药物相互作用
结合P-gp和强或中等CYP3A诱导剂：避免同时使用。
联合P-gp和强CYP3A抑制剂：更频繁地监测患者的NUBEQA不良反应。
BCRP底物：尽可能避免同时使用BCRPs底物的药物。如果一起使用，更频繁地监测患者的不良反应并考虑降低BCRP底物药物的剂量。
用于特定人群
严重肾功能损害（不是血液透析）：建议剂量为每天两次300毫克。
中度肝功能损害：建议剂量为每天两次300毫克。
包装提供/存储和处理
提供
NUBEQA（darolutamide）300毫克薄膜包衣片剂为白色至灰白色椭圆形片剂，一面标有“300”，另一面标有“BAYER”。NUBEQA 300毫克片剂有120片装。
NDC 50419-395-01
存储和处理
储存在20°C至25°C（68°F至77°F）; 允许的偏差在15°C至30°C（59°F至86°F）之间[参见USP ControlledRoom Temperature]。
首次打开后保持瓶子紧闭。
完整说明附件：
http://labeling.bayerhealthcare.com/html/products/pi/Nubeqa_PI.pdf
NUBEQA(darolutamide) tablets, for oral use
Initial U.S. Approval: 2019
IMPORTANT SAFETY INFORMATION
It is not known if NUBEQA is safe and effective in women and children. NUBEQA can harm unborn babies and cause loss of pregnancy. Men with female partners who may become pregnant should use birth control (contraception) during treatment and for 1 week after the last dose of NUBEQA。
INDICATION
NUBEQA(darolutamide) tablets is a prescription medicine used to treat men with prostate cancer that has not spread to other parts of the body and no longer responds toamedical or surgical treatment that lowers testosterone.
IMPORTANT SAFETY INFORMATION
It is not known if NUBEQA is safe and effective in women and children. NUBEQA can harm unborn babies and cause loss of pregnancy. Men with female partners who may become pregnant should use birth control (contraception) during treatment and for 1week after the last dose of NUBEQA.
Before taking NUBEQA, tell your healthcare provider about all your medical conditions, including if you:
have kidney or liver problems
are pregnant or plan to become pregnant. NUBEQA can cause harm to your unborn baby and loss of pregnancy (miscarriage)
have a partner who may become pregnant. Males who have female partners who may become pregnant should use effective birth control (contraception) during treatment and for 1 week after the last dose of NUBEQA. Talk with your healthcare provider about birth control methods.
are breastfeeding or plan to breastfeed. It is not known if NUBEQA passes into breast milk.
Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. NUBEQA may affect the way other medicines work and other medicines may affect how NUBEQA works.
You should not start or stop any medicine without talking to your healthcare provider that prescribed NUBEQA.
Most common side effects of NUBEQA include:
Feeling more tired than usual
Arm, leg, hand, and foot pain
Rash
Decreased white blood cells (neutropenia)
Changes in tests that determine how your liver works (liver function tests)