近日，抗癌新药Faslodex已被批准用于治疗激素受体阳性转移性乳腺癌。适用于接受抗雌激素治疗（如他莫昔芬）后疾病进展的绝经后妇女。治疗是每月一次的肌内注射。
批准日期：2016年3月2日 公司：阿斯利康
FASLODEX(氟维司群[fulvestrant])注射，肌肉内的使用
美国最初批准:2002年
最近的重大变化
适应症和用法:11/2017
剂量和管理:11/2017
作用机制
许多乳腺癌都有雌激素受体(ER)，这些肿瘤的生长可以被雌激素刺激。Fulvestrant是一种雌激素受体拮抗剂，它以一种竞争性的方式与雌激素受体结合，其亲和力与雌二醇相当，并下调了人类乳腺癌细胞中的ER蛋白。
体外研究表明，fulvestrant是一种可逆的抑制他莫昔芬耐药和雌激素敏感性人类乳腺癌(MCF-7)细胞系生长的抑制剂。在体内肿瘤研究中，fulvestrant延迟了人乳腺癌MCF-7细胞异种移植的肿瘤的建立。Fulvestrant抑制了已建立的MCF-7异种移植和耐他莫昔芬乳腺肿瘤异种移植的生长。
在未成熟或切除卵巢的小鼠和大鼠体内，福韦特伦没有显示出阿格尼特型效应。在未成熟大鼠和切除卵巢的猴子体内的研究中，富伐他汀阻断了雌二醇的子宫增生性作用。在绝经后的妇女中，对于fulvestrant治疗(每月250毫克)，血浆中FSH和LH的浓度没有变化，表明没有外周类固醇效应。
适应症和用法
FASLODEX是一种雌激素受体拮抗剂
•激素受体(HR)阳性，人类表皮生长因子受体2 (HER2)阴性的晚期乳腺癌治疗绝经后未接受内分泌治疗的妇女。
•在内分泌治疗后病情进展的绝经后妇女中，hr-阳性晚期乳腺癌的治疗。
•在内分泌治疗后病情进展的女性中，HR-positive, HER2-negative advanced or metastatic breast cancer合并palbociclib或abemaciclib治疗。
剂量和管理
•FASLODEX 500mg应缓慢地肌注入臀部(臀区)(每次注射1-2分钟)，每次注射2次，每次5毫升，第1天，第15天，第29天，此后每月注射一次。
•建议中度肝损害患者服用250毫克的剂量，缓慢(1-2分钟)肌注臀部(臀区)，第1、15、29天注射一次5毫升，此后每月注射一次。
剂型及强度
FASLODEX是一种肌肉注射剂，以250毫克/5毫升的剂量提供。
禁忌症
•过敏症。
警告和预防措施
•出血风险:有出血倾向、血小板减少或抗凝药物使用的患者慎用。
•增加肝损害患者暴露量:中度肝损害患者使用250mg剂量。
•注射部位反应:由于坐骨神经靠近，在臀背注射部位使用筋膜曲张时要小心。
•胚胎-胎儿毒性:可导致胎儿伤害。建议女性注意生殖潜能和对胎儿的潜在风险，并采取有效的避孕措施。
•血清雌二醇的免疫测定:FASLODEX可以通过免疫测定干扰雌二醇的测定，导致雌二醇水平错误升高。
不良反应
•最常见的不良反应发生在≥5%的病人接受FASLODEX 500毫克是:注射部位疼痛、恶心、骨痛、关节痛、头痛、背痛、疲劳、肢体疼痛,潮热,呕吐,厌食,乏力,肌肉骨骼疼痛,咳嗽,呼吸困难,便秘。
•15%的FASLODEX患者出现肝酶升高(ALT, AST, ALP)，且不依赖剂量。
药物的相互作用
•没有已知的药物-药物相互作用。
用于特定人群
哺乳期:建议不要哺乳。
包装提供/存储和处理
FASLODEX蛋白以两个5毫升的透明中性玻璃(1型)桶提供，每个桶包含250毫克/5毫升的肌注FASLODEX蛋白溶液，并配有明显的填塞物。
NDC 0310-0720-10
并给出了注射器与聚苯乙烯盘柱塞杆和安全针(SafetyGlide™)连接到桶。
储存:
冷藏2°8°C (-46°F 36°)。为防光，保存在原来的纸箱，直到使用时间。
完整资料附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=83d7a440-e904-4e36-afb5-cb02b1c919f7
FASLODEX works in HR-positive breast cancer cells by targeting a special receiver called the estrogen receptor, which can play an important role in advanced HR-positive breast cancer. Estrogen is a hormone that can connect with the estrogen receptor and send signals leading to the growth of cancer. Taking FASLODEX may decrease the potential for cancer growth by interrupting these signals.
IMPORTANT SAFETY INFORMATION
You should not receive FASLODEX if you have had an allergic reaction to fulvestrant or any of the ingredients in FASLODEX. Talk to your health care provider if you experience symptoms of an allergic reaction to FASLODEX, which may include itching or hives; swelling of your face, lips, tongue, or throat; and trouble breathing.
Before receiving FASLODEX, tell your health care provider about all of your medical conditions, including if you:
Have a low level of platelets in your blood or bleed easily. Especially tell your health care provider if you take a blood thinner medicine (anticoagulant)
Have liver problems
Are pregnant or plan to become pregnant, because FASLODEX can harm your unborn baby. Women who are able to become pregnant should use effective birth control during treatment with FASLODEX and for 1 year after the final dose. Tell your health care provider right away if you become pregnant or think you are pregnant while on FASLODEX
Are breastfeeding or plan to breastfeed. It is not known if FASLODEX passes into breast milk. Do not breastfeed during treatment with FASLODEX and for 1 year after the final dose. Talk to your health care provider about the best way to feed your baby during this time
Tell your health care provider about all of the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. FASLODEX may affect the way other medicines work, and other medicines may affect how FASLODEX works.

FASLODEX is administered by your health care provider as an injection into the muscle of each buttock. Your health care provider may change your dose of FASLODEX if needed.
FASLODEX may cause injection site–related nerve damage. Call your health care provider if you develop any of the following symptoms in your legs following a FASLODEX injection: numbness, tingling, or weakness.
Common side effects of FASLODEX include injection site pain; nausea; muscle, joint, and bone pain; headache; tiredness; hot flashes; vomiting; loss of appetite; weakness; cough; shortness of breath; constipation; increased liver enzymes; and diarrhea.
Tell your health care provider if you have any side effect that bothers you or does not go away. These are not all of the possible side effects with FASLODEX. For more information, ask your health care provider or pharmacist. You may report side effects to the FDA at 1-800-FDA-1088.
Approved Uses for FASLODEX
FASLODEX is a prescription medicine used to treat women with:
Hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced breast cancer, who have gone through menopause and have not been previously treated with endocrine therapy
HR-positive advanced breast cancer, who have gone through menopause and whose disease has progressed after endocrine therapy
HR-positive, HER2‐negative advanced breast cancer or breast cancer that has spread to other parts of the body (metastatic), in combination with palbociclib or abemaciclib, in women whose disease has progressed after endocrine therapy
When FASLODEX is used in combination with palbociclib, please also see the palbociclib Patient Information.
When FASLODEX is used in combination with abemaciclib, please also see the abemaciclib Patient Information.
It is not known if FASLODEX is safe and effective in children or in people with severe liver problems.