制造商：
葛兰素史克制药

药理分类：
溶细胞单克隆抗体（CD20的指导）

活性成分（补）：
Ofatumumab 20mg/mL;稀释后的第四输液水溶液，不含防腐剂。

指示（补）：
慢性淋巴细胞白血病（CLL）耐火材料氟达拉滨和阿来组单抗。

药理：
Ofatumumab，一个细胞毒性IgG1k人源单克隆抗体，同时结合具体的小和CD20分子胞外大循环。在CD20分子的表达正常的B淋巴细胞（前B -成熟B淋巴细胞）和B细胞慢性淋巴细胞白血病。在CD20分子是不见棺材不流从细胞表面，而不是内在以下抗体结合。

绑定的ofatumumab晶圆厂域的CD20分子和FC域介导的免疫效应的功能，造成乙体外细胞裂解。数据表明，细胞溶解的可能机制包括补体依赖的细胞毒性和抗体依赖细胞介导的细胞毒作用。

该产品的批准是基于持久客观反应示威，没有数据显示，在疾病相关症状改善或增加的生存。难治性与慢性淋巴细胞白血病的氟达拉滨和阿来组单抗的患者，在循环CD19阳性的B细胞中位数下降91输液的第8和第12输注85％％。对淋巴细胞的恢复时间，包括CD19阳性的B细胞，到正常水平尚未确定。

Ofatumumab是淘汰既是一个目标，独立的航道和B细胞介导的途径。由于B细胞耗竭，大大降低了ofatumumab随后注入清理后比第一输液。

临床试验：
在ofatumumab疗效研究的单臂，多中心研究，涉及154复发或难治性慢性淋巴细胞白血病患者。
Oftamumab四是管理的输液按照时间安排如下：300毫克（周0），2000mg每周7输液（周1至7）和2000mg，每4周注射4（周12至24）。人口的疗效包括慢性淋巴细胞白血病病人的耐火材料氟达拉滨和阿来组单抗。药物耐火度被界定为未能取得至少部分反应或疾病进展的6个月内，对氟达拉滨或阿来组单抗最后剂量。主要疗效持久的客观结果是肿瘤反应率。调查人员确定的，与氟达拉滨的患者的总有效率和阿来组单抗耐药性cll为42％，以中位数的6.5个月反应。没有完整的答复。抗肿瘤活性中也有所体现在这名病人的研究和多中心，开放标签剂量递增研究复发或难治性慢性淋巴细胞白血病患者进行。

法律分类：
接收

成人：
与对乙酰氨基酚Premedicate（口服），抗组织胺（口头或四），皮质类固醇（四）见文献。由四输注给（使用在线过滤器;率与剂量输注期间不同）。最初300毫克一次，然后一周后2000mg每周7剂量，然后4周后2000mg，每4周为4剂。

儿童：
不建议。

预防措施（补）：
央行监测，血小板，和神经的变化。预乙肝屏幕高风险患者;停止病毒性肝炎如果出现。妊娠（Cat.C）。哺乳母亲。

互动（补）：
避免与活病毒疫苗接种。

不良反应（补）：
中性粒细胞，血小板减少，贫血，肺炎，发热，咳嗽，疲劳，呼吸困难，皮疹，胃肠不适，支气管炎，上呼吸道感染，输液反应（如支气管痉挛，喉，肺，或血管性水肿，潮红，超或低血压，昏厥，心肌缺血，背部或腹部疼痛，发烧，荨麻疹）（中断输液和监测;如果不重新启动反应发生4级），多灶性脑白质病（如发生中断和监测），肠梗阻，感染（如败血症）。

如何提供：
单用小瓶（毫升）-3，10

Arzerra™ Product Overview
Arzerra™ (ofatumumab) is indicated for the treatment of chronic lymphocytic leukaemia (CLL) in adult patients who are refractory to fludarabine and alemtuzumab.
Administration and Dosage of Arzerra™:
Arzerra™is available in  two pack sizes:
• Pack of 3 vials x 5 ml (100 mg/5ml) – unchanged vial size [1]
• Pack of 1 vial x 50 ml (1,000 mg/50ml) – new vial size  [2]
Arzerra™ should be administered by a physician experienced in the use of cancer medicines and where full resuscitation facilities are immediately available.
The recommended dose is 300 mg Arzerra™ for the first infusion and 2,000 mg Arzerra™ for all subsequent infusions.
For further information, please see the Administration section.
Arzerra™How does it work?
Arzerra™  is a human monoclonal antibody (IgG1) that binds specifically to a distinct epitope encompassing both the small and large extracellular loops of the CD20 molecule, leading to complement-dependent and antibody-dependent cell-mediated cytotoxicity and lysis of tumour cells . In the final analysis of the pivotal single arm open label study, the overall response rate following Arzerra™  treatment, in patients refractory to fludarabine and alemtuzumab, was 51% (95% CI: 40, 60), and the median overall survival was 14.2 months (95% CI:  9.8, 20.4).
Contraindications of Arzerra™:
Arzerra™ is contraindicated in patients who demonstrate hypersensitivity to Arzerra™ or to any excipients.
For further information on ofatumumab, please see the Arzerra™ SPC.
GLAXO GRP LTD

Manufacturer:
GlaxoSmithKline Pharmaceuticals
Pharmacological Class:
Cytolytic monoclonal antibody (CD20-directed)Active Ingredient(s):
Ofatumumab 20mg/mL; soln for IV infusion after dilution;
preservative-free.
      

Indication(s):
Chronic lymphocytic leukemia(CLLrefractorytofludarabine and alemtuzumab.
Pharmacology:
Ofatumumab, a cytolytic IgG1k human monoclonalantibody, binds specifically to both the small and the large extracellular loops of the CD20 molecule.
The CD20 molecule is expressed on normal B lymphocytes (pre-B- to mature B-lymphocytes) and on B-cell CLL. The CD20 molecule is not shed from the cell surface and is not internalized following antibody binding.
The Fab domain of ofatumumab binds to the CD20molecule, and the Fc domain mediates immune effector functions, causing B-cell lysis in vitro. Data suggests that possible mechanisms of cell lysis include complement-dependent cytotoxicity and antibody-dependent, cell-mediated cytotoxicity.
The approval of thisproductwasbaseduponthedemonstration of durable objective responses; no data have shown an improvement in disease related symptoms or increased survival. In patients with CLL refractory tofludarabine and alemtuzumab, the median decrease in circulating CD19-positive B cells was 91% with the 8th infusion and 85% with the 12th infusion. The time to recovery of lymphocytes, including CD19-positive B cells, to normal levels has not been determined.
Ofatumumab is eliminated through both a target-independent route and a B-cell mediated route. Due to the depletion of B cells, the clearance of ofatumumab decreases substantially after subsequent infusions compared to the first infusion.

Clinical Trials:
The efficacy of ofatumumab was examined in a single-arm, multicenter study involving 154 patients with relapsed or refractory CLL. Oftamumab was administered by IV infusion according to the following schedule: 300mg (Week 0), 2000mg weekly for 7 infusions (Weeks 1 through 7) and 2000mg every 4 weeks for 4 infusions (Weeks 12 through 24). The efficacy population was comprised of patients with CLL refractory tofludarabine and alemtuzumab. Drug refractoriness was defined as failure to achieve at least a partial response to, or disease progression within 6 months of, the last dose of fludarabine or alemtuzumab. The main efficacy outcome was durable objective tumor response rate. Theinvestigator-determined overall response rate in patients with fludarabine- and alemtuzumab-refractory CLL was 42%, with a median response of 6.5months. There were no complete responses. Antitumor activity was also seen in additional patients in this study and in a multicenter, open-label dose-escalation study conducted in patients with relapsed or refractory CLL.
Legal Classification:
Rx
Adults:
Premedicate with acetaminophen (oral), antihistamine (oral or IV), corticosteroid (IV); see literature. Give by IV infusion (use in-line filter; rate varies with dose and during infusion). Initially 300mg once, then 1 week later 2000mg weekly for 7 doses, then 4 weeks later 2000mg every 4 weeks for 4 doses.
Children:
Not recommended.
      
Precaution(s):
Monitor CBC, platelets, and for neurological changes. Pre-screen for hepatitis B in high-risk patients; discontinue if viral hepatitis emerges.
Pregnancy (Cat.C). Nursing mothers.
Interaction(s):
Avoid vaccination with live viral vaccines.
Adverse Reaction(s):
Neutropenia, thrombocytopenia,anemia,pneumonia,pyrexia, cough, fatigue, dyspnea, rash, GI upset, bronchitis, upper respiratory tract infections;
infusion reactions (eg, bronchospasm; laryngeal, pulmonary, or angioedema;
flushing, hyper- orhypotension,syncope,cardiacischemia, back or abdominal pain, fever, urticaria) (interrupt infusion and monitor; do not restart if grade 4reaction occurs), progressive multifocal leukoencephalopathy (discontinue ifoccursandmonitor),intestinalobstruction, infections (eg, sepsis).

How Supplied:
Single-use vial (5mL)—3, 10

Last Updated:
Arzerra（ofatumumab）
ARZERRA

单克隆抗体Arzerra获准用于难治性慢性淋巴细胞白血病
      
2009年10月26日，美国食品药品管理局（FDA）通过加速审批程序批准Arzerra (ofatumumab) 用于氟达拉滨（fludarabine）和阿伦单抗（alemtuzumab）治疗无效的慢性淋巴细胞白血病(CLL)患者。

Arzerra是一种可以引起免疫应答以对抗正常和恶性B细胞的单克隆抗体。其附着于名为CD20蛋白分子上的大小环状表位。CD20存在于B细胞表面，而这样的细胞在CLL中呈现为恶性。
 
FDA的加速审批程序指出，该药需要进行进一步的研究。该药品生产厂商最近进行了一个CLL患者的临床试验，证实了标准化疗联合Arzerra延迟了疾病发展的进程。
Arzerra的有效性在其他疗法治疗无效的59名CLL患者身上得到了评估。而该药的安全性在两项共包括181位癌症患者的研究中进行了评估。该药报道的常见副作用包括：肺炎、发热、咳嗽、腹泻、疲乏、气短、皮疹、恶心、支气管炎、上呼吸道感染以及正常白细胞和红细胞计数降低。
 
Arzerra最严重的副作用是增加了感染的机会。在Arzerra治疗前和治疗过程中需要筛查乙型肝炎感染的高危患者。在治疗前后，需要监控确诊为非活动期传染性肝炎患者体内病毒感染再激活情况。此外尚有发生致命性疾病——进行性多灶性脑白质病的危险。

---------------------------------------------------------------
原产地英文商品名:
ARZERRA 1000MG/50ML/VIAL
原产地英文药品名:
OFATUMUMAB
中文参考商品译名:
ARZERRA 1000毫克/50毫升/瓶
中文参考药品译名:
单克隆抗体
生产厂家中文参考译名:
葛兰素史克
生产厂家英文名:
GLAXO GRP LTD

---------------------------------------------------------------
原产地英文商品名:
ARZERRA 100MG/50ML/VIAL
原产地英文药品名:
OFATUMUMAB
中文参考商品译名:
ARZERRA 100毫克/5毫升/瓶
中文参考药品译名:
单克隆抗体
生产厂家中文参考译名:
葛兰素史克
生产厂家英文名:
GLAXO GRP LTD