近日，美国FDA已批准皮下注射剂型（SC）Benlysta（belimumab，贝利木单抗），用于正在接受标准治疗的活动性、自身抗体阳性系统性红斑狼疮（SLE）成人患者。SLE是最常见的狼疮类型，约占全部狼疮病例的70%，这是一种慢性、无法治愈的自身免疫性疾病，患者体内产生自身抗体攻击机体任何一个组织。此次批准，也标志着治疗SLE的首个皮下注射药物获批。
Benlytsa（贝利木单抗）是近50多年来获批治疗SLE的首个新药。在美国和欧盟，静脉注射剂型（IV）Benlysta于2011年获批上市，用于自身抗体阳性的SLE成人患者。目前，Benlysta通过静脉输注给药，每4周输注一次，剂量根据体重调整（10mg/kg），耗时约1个小时。
皮下注射剂型Benlysta则通过皮下注射给药，产品有2种形式：单剂量预灌封注射器和单剂量自动注射器，患者通过培训后可自行皮下注射给药，该剂型将为SLE患者群体提供一种重要的治疗选择。
批准日期：2017年7月24日  公司：葛兰素史克
BENLYSTA（贝利木单抗 belimumab），用于注射，静脉内使用
BENLYSTA（贝利木单抗 belimumab）注射剂，皮下使用
最初美国批准：2011
目前的主要变化
用法用量给药，皮下给药说明：07/2017
警告和注意事项：07/2017
作用机理
BENLYSTA是BLyS的特异性抑制剂阻断可溶性BLyS的结合，一个B细胞存活因子，其在B细胞上的受体。BENLYSTA不直接结合的B细胞，但通过结合的BLyS，BENLYSTA抑制B细胞的存活，包括自身反应性B细胞，并减少B细胞分化成产生免疫球蛋白的浆细胞。
适应症和用法
BENLYSTA是B淋巴细胞刺激因子（BLyS）特异性抑制剂，其用于治疗成人活性，自身抗体阳性，系统性红斑狼疮谁正在接受标准治疗的治疗中。
使用限制：BENLYSTA的疗效尚未重症狼疮性肾炎，重度活动性中枢神经系统狼疮BENLYSTA还没有与其他生物或BENLYSTA的环磷酰胺静脉使用组合进行研究评估在这些情况下，不建议。
用法用量
静脉注射
•10mg/kg的在2周的时间间隔为所述第一3个剂量，并在4周的时间间隔之后。重新构建，稀释，和管理作为静脉内输注1小时内的。
•考虑针对输液反应和过敏反应预防给药前用药。
皮下注射
•200毫克，每周一次。
剂型和规格
静脉输液
注射：120毫克或400毫克单剂量小瓶中静脉内输注前冻干粉末用于重构和稀释。
皮下注射
注射剂：200毫克/毫升的单剂量预填充自动注射器或单剂量预充式注射器。
禁忌症
上一页过敏反应到贝利木单抗。
警告和注意事项
•死亡率：有在临床试验的对照期报道BENLYSTA比安慰剂更多的死亡。
•严重感染：严重，有时甚至致命的感染已报告重症患者或慢性感染接受免疫抑制剂，包括BENLYSTA使用谨慎的患者请考虑中断与BENLYSTA治疗，如果患者BENLYSTA治疗期间制定新的感染。
•进行性多灶性白质脑病（PML）:患者新发或呈现恶化的神经症状和体征，应为PML通过合适的专科医生如果PML证实，考虑免疫抑制剂治疗，包括BENLYSTA停药评估。
•过敏反应，包括过敏性休克：.严重和致命的反应已报告BENLYSTA静脉内使用应准备处理过敏反应期间和BENLYSTA的静脉给药后的适当时间监视患者的医疗保健机构进行管理。
•抑郁:.抑郁症和自杀都与BENLYSTA患者的试验被报道，应指导联系他们的卫生保健提供者，如果他们遇到新的或恶化抑郁，自杀的想法，或其他情绪变化。
•免疫：活疫苗不应与BENLYSTA同时给予。
不良反应
•常见不良反应（≥5％）：恶心，腹泻，发热，鼻咽炎，支气管炎，失眠，疼痛下肢，抑郁症，偏头痛，咽炎，和注射部位反应（皮下给药）。
包装规格/储存与处理
静脉输液
BENLYSTA（贝利木单抗），用于注射的无菌，无防腐剂，冻干用于在单剂量的玻璃小瓶中设置有橡胶塞（未与天然橡胶胶乳制成）和翻盖关闭密封静脉输注前重构和稀释粉末。每个5姆·维尔含有120毫克贝利木单抗，每一20毫升管形瓶包含400mg的贝利木单抗的。
BENLYSTA小瓶被提供如下：
120毫克在一个5毫升的单剂量小瓶贝利单抗（NDC 49401-101-01）
400毫克在20-mL的单剂量小瓶贝利单抗（NDC 49401-102-01）
在原始纸箱直到使用以避光2°至8°C（36°〜46°F）。储存小瓶冷藏小瓶中。不要冷冻，避免暴露于热。
皮下注射
BENLYSTA（贝利木单抗）注射是清楚的乳白色和无色至浅用于皮下使用的黄色溶液。每个单剂量预填充自动注射器或单剂量预充式注射器被设计为在1毫升的溶液递送200mg的贝利木单抗的并作为如下：
200毫克/以4:1的纸箱具有连接27号，半英寸针毫升单剂量预充式自动注射器（NDC 49401-088-01）（NDC 49401-088-35）。
200毫克/英寸4纸箱毫升单剂量预充式玻璃注射器附接27号，半英寸针（NDC 49401-088-42）（NDC 49401-088-47）。
冷藏的预充式自动注射器，并在2℃下的预充式注射器中，以8℃（36°F至46°F），保持该产品在原纸箱从光保护直到使用的时候，不要冻结。不要摇晃，避免暴露在热。
BENLYSTA可以保存在冰箱中的外侧用于在原来的容器达12小时86°F（30℃）。不要使用，并且如果为12小时以上遗漏不放回冰箱放置。
完整处方资料附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2fa3c528-1777-4628-8a55-a69dae2381a3
BENLYSTA (belimumab) injection, for subcutaneous
BENLYSTA is a prescription medication used to treat adults with active systemic lupus erythematosus (SLE or lupus) who are receiving other lupus medicines.
It is not known if BENLYSTA is safe and effective in people with severe active lupus nephritis or severe active central nervous system lupus, and it has not been studied in combination with other biologics or intravenous cyclophosphamide. Use of BENLYSTA is not recommended in these situations.
Do not receive BENLYSTA if you are allergic to belimumab or to any of the ingredients in BENLYSTA.
Important Safety Information
The most important information to know about BENLYSTA
BENLYSTA can cause serious side effects. Some of these side effects may cause death. It is not known if BENLYSTA causes these serious side effects.
Tell your healthcare provider right away if you have any of the symptoms listed below while receiving BENLYSTA
•Infections: Symptoms can include fever, chills, pain or burning with urination, urinating often, coughing up mucus, shortness of breath, or warm, red or painful skin on your body.
•Heart problems: Symptoms can include chest discomfort or pain, shortness of breath, cold sweats, nausea, dizziness, or discomfort in other areas of the upper body.
•Allergic (hypersensitivity) reactions: Serious allergic reactions can happen on the day of, or in the days after, receiving BENLYSTA and may cause death. Tell your healthcare provider right away if you have any of the following symptoms of an allergic reaction: itching, swelling of the face, lips, mouth, tongue, or throat, trouble breathing, anxiousness, low blood pressure, dizziness or fainting, headache, nausea, or skin rash.
•Mental health problems and suicide: Symptoms can include thoughts of suicide or dying, attempt to commit suicide, trouble sleeping, new or worse anxiety or depression, acting on dangerous impulses, other unusual changes in your behavior or mood, or thoughts of hurting yourself or others.
Before receiving BENLYSTA also discuss with your healthcare provider if you:
•think you have an infection or have infections that keep coming back. You should not receive BENLYSTA if you have an infection unless your healthcare provider tells you to.
•have or have had mental health problems such as depression or thoughts of suicide.
•have recently received a vaccination or if you think you may need a vaccination. If you are receiving BENLYSTA, you should not receive live vaccines.
•are taking other medicines, including prescription and over-the-counter medicines, vitamins, and herbal supplements.
•are allergic to other medicines.
•are receiving other biologic medicines, monoclonal antibodies, or IV infusions of cyclophosphamide (CYTOXAN®).
•have or have had any type of cancer.
•have any other medical conditions.
•are pregnant or plan to become pregnant. It is not known if BENLYSTA will harm your unborn baby. Tell your healthcare provider if you become pregnant during your treatment with BENLYSTA. If you are able to become pregnant, you should talk to your healthcare provider about whether or not to use birth control (contraception) and receive BENLYSTA. If BENLYSTA is recommended, you should use an effective method of birth control while receiving BENLYSTA and for at least 4 months after the final dose of BENLYSTA. If you become pregnant while receiving BENLYSTA, talk to your healthcare provider about enrolling in the BENLYSTA Pregnancy Registry. You can enroll in this registry by calling 1-877-681-6296. The purpose of this registry is to monitor the health of you and your baby.
•are breastfeeding or plan to breastfeed. It is not known if BENLYSTA passes into your breast milk. You and your healthcare provider should talk about whether or not you should receive BENLYSTA and breastfeed.
Possible side effects of BENLYSTA
•Progressive multifocal leukoencephalopathy (PML). PML is a serious and life-threatening brain infection. Your chance of getting PML may be higher if you are treated with medicines that weaken your immune system, including BENLYSTA. PML can result in death or severe disability. If you notice any new or worsening medical problems such as those below, tell your healthcare provider right away: memory loss, trouble thinking, dizziness or loss of balance, difficulty talking or walking, or loss of vision.
•Cancer. BENLYSTA may reduce the activity of your immune system. Medicines that affect the immune system may increase your risk of certain cancers.
The most common side effects of BENLYSTA are nausea, diarrhea, fever, stuffy or runny nose and sore throat, cough, trouble sleeping, leg or arm pain, depression, headache, and pain, redness, itching, or swelling at the site of injection. These are not all the possible side effects of BENLYSTA. Call your doctor for medical advice about side effects.
Other Important Information
In 2 of 3 studies, fewer blacks/African Americans who received BENLYSTA responded to treatment compared to blacks/African Americans who did not receive BENLYSTA. Consult with your healthcare provider to determine if BENLYSTA is right for you.