制造商：
葛兰素史克制药
药理分类：
溶细胞的单克隆抗体（CD20的定向）
活性成分（补）：
Ofatumumab 20mg/mL;溶液稀释后的静脉输液，不含防腐剂。
指示（补）：
慢性淋巴细胞白血病（CLL）的难治性氟达拉滨和alemtuzumab。
药理作用：
Ofatumumab一个杀伤IgG1k人单克隆抗体，同时结合具体的小型和大型的CD20分子胞外循环。在抗CD20分子表达于正常的B淋巴细胞（预B对成熟B淋巴细胞）和B细胞慢性淋巴细胞白血病。的抗CD20分子是不是从细胞表面脱落并没有内在下面抗体结合。
晶圆厂的ofatumumab结合域的CD20分子，和促委会功能结构域介导的免疫效应，造成体外B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作用和抗体依赖细胞介导的细胞毒作用。
该产品的批准是基于目标的持久反应，示威的任何数据都显示出在疾病相关的症状或提高生存率的改善。根据CLL患者耐火材料氟达拉滨和alemtuzumab，在循环CD19的阳性B细胞减少的91％中位数的8输液，85％的第十二届输液。对复苏的淋巴细胞，包括CD19的阳性B细胞，到正常水平的时间尚未确定。
Ofatumumab是消灭一个目标既独立路线和B -细胞介导的途径。由于B细胞耗竭，ofatumumab在随后的清理大幅减少输液比第一输液。
临床试验：
对ofatumumab疗效观察了单手臂，多中心的研究涉及154例复发或难治性慢性淋巴细胞白血病患者。 Oftamumab通过静脉输注给药按照时间安排如下：300毫克（0周），为2000mg为7输液（周1到7），并为2000mg每4周注射4（12到24周），每周一次。人口构成的疗效与慢性淋巴细胞白血病患者难治性氟达拉滨和alemtuzumab。药物难治性定义为未能实现在6时，阿仑单抗的最后剂量氟达拉滨个月或至少部分反应或病情恶化。主要效果结果是持久的客观肿瘤反应率。调查人员，确定病人的整体回应率氟达拉滨和阿仑单抗-耐火材料白血病是42％之间，中位数的6.5个月响应。目前还没有完整的答复。抗肿瘤活动也出现在其他病人在这项研究中的多中心开放标记剂量升级研究与治疗复发或难治性慢性淋巴细胞白血病患者中进行。
法律分类：
接收
成人：
Premedicate与对乙酰氨基酚（口服），抗组织胺（口服或静脉注射），皮质类固醇（四）见文献。通过静脉注射给予（使用在线过滤器;率剂量输注异）。最初300毫克一次，然后一周后，7剂量为2000mg，然后按4周后剂量为2000mg，每4 4周。
儿童：
不推荐。
警告/注意事项：
监测血常规，血小板和神经系统的变化。预先筛选乙肝高危患者;如果停止病毒性肝炎出现。妊娠（Cat.C）。哺乳的母亲。
互动（补）：
避免与活病毒疫苗接种。
不良反应（补）：
白细胞减少，血小板贫血，肺炎，发烧，咳嗽，疲劳，喘，皮疹，胃肠心烦，支气管炎和上呼吸道感染;输液反应（如气管痉挛;喉癌，肺，或血管性水肿;冲洗，超或性低血压，昏厥，心脏缺血，背部和腹部疼痛，发热，风疹）（中断输液和监测;如果不重新启动四级反应发生），进行性多灶性白质脑病（如果发生中断和监督），肠道阻塞，感染（如败血症）。
如何提供：
单用小瓶（5毫升）-3，10
最后更新：
2010年2月25日
ARZERRA
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 (CLL) refractory to fludarabine and alemtuzumab.
Pharmacology:
Ofatumumab, a cytolytic IgG1k human monoclonal antibody, 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 CD20 molecule, 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 this product was based upon the demonstration of durable objective responses; no data have shown an improvement in disease related symptoms or increased survival. In patients with CLL refractory to fludarabine 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 to fludarabine 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. The investigator-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.
Warnings/Precautions:
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- or hypotension, syncope, cardiac ischemia, back or abdominal pain, fever, urticaria) (interrupt infusion and monitor; do not restart if grade 4 reaction occurs), progressive multifocal leukoencephalopathy (discontinue if occurs and monitor), intestinal obstruction, infections (eg, sepsis).
How Supplied:
Single-use vial (5mL)—3, 10