简介：

部份中文泽娃灵处方资料（仅供参考）
治疗类别名称
抗肿瘤剂，放射标记的抗CD20单克隆抗体
欧文商標名
Zeva lin yttrium injection
一般名：イブリツモマブ　チウキセタン（遺伝子組換え）
一般名：（欧名） Ibritumomab Tiuxetan（genetical recombination）
分子量：148kDa（daltons）
放射性核種の特性 90Yとして
物理化学的半減期：64.1時間
ベータ線エネルギー：2.281MeV（99.98％）
減衰表経過時間
（時間）残存放射能
（％）
本質
重链（γ1链）和轻链213的氨基酸残基通过一个cDNA的表达在中国仓鼠卵巢细胞中产生的一个的IgG1的编码（κ链）是小鼠抗人CD20单克隆抗体（C1018H1564N276O333S7;分子量：23,221.42轻链2分子和445个氨基酸残基组成的）（C2183H3334N564O671S21;分子量：48,888.57）糖蛋白的重链组成的两个分子氮组成 -  {（2S）-2- [双（羧甲基）氨基]3-（4-异硫氰酸根合 - 苯基）丙基}-N- {2- [双（羧甲基）氨基]丙基}甘氨酸（C23H30N4O10S;分子量：554.57）与被结合到（重组的）一个修饰的糖蛋白一。
审批条件
由于临床试验的情况下在日本是非常有限的，上市后，直到一定数量案件的数据被集成，通过实施的所有情况下，使用效果的调查，钇（ 90Y）替伊莫单抗（基因重组）以及了解病人的背景信息，钇（收集早期中的安全和90Y的功效）替伊莫单抗（基因重组），钇（90 Y）替伊莫单抗数据采取必要措施，正确使用（转基因）。
药效药理
CD20抗原
人CD20抗原，原B细胞，是几乎所有的这些表达于正常和致瘤性B细胞除浆细胞（磷蛋白）分化抗原，细胞比B细胞的其他不表达。
抗肿瘤作用
钇中时与（重组）施用移植拉莫斯肿瘤细胞（90Y）替伊莫单抗的小鼠肿瘤模型中，观察到杀肿瘤作用（体内）。
作用机序
替伊莫显示了在B细胞上[4] CD20抗原的强烈的抗原特异性的亲和力。 （强结合90Y和）单抗是螯合剂共价结合到暴露的赖氨酸氨基和精氨酸中的抗体。钇（90Y）替伊莫单抗（基因重组），利妥昔单抗结合至（遗传重组）以及CD20抗原，通过从诱导和凋亡90Y的β射线辐射，以诱导细胞毒性。
适应症
CD20阳性复发或以下疾病难治
低档B细胞非何杰金氏淋巴瘤，套细胞淋巴瘤
用法用量
注射溶液制备用于该组的无菌小瓶制备注射溶液的醋酸钠溶液的适当量，并把氯化钇（90Y）溶液1500MBq，这是通过加入替伊莫单抗溶液1.3毫升，注射溶液制备的适当量的缓冲液混合此外，该解决方案是钇（90Y）替伊莫单抗（遗传重组）注射。 （请参见“关于申请注意事项”）
通常情况下，成人，利妥昔单抗（基因重组）静脉输注后，迅速，静脉给药超过14.8MBq /公斤（最高1184MBq）步行10分钟钇（90Y）替伊莫单抗（基因重组） 。另外，在11.1MBq /公斤的减少，这取决于患者的状况。
顺便说一下，钇（90 Y）替伊莫单抗（遗传重组）之前，注射溶液的施用，并且确认替伊莫单抗（遗传重组）的整合位点，以检查异常的生物分布。
包装
泽娃灵钇（90Y），用于静脉注射设定
1套
制造商（进口）
光谱制药有限责任公司
Zeva lin (ibritumomab tiuxetan)
Company: Biogen IDEC
Approval Status: Approved February 2002
Treatment for: Non-Hodgkin's lymphoma
Areas: Oncology
General Information
In February 2002, Zeva lin was the first radioimmunotherapy to receive FDA approval. Zeva lin is indicated for the treatment of relapsed or refractory low grade, follicular, or transformed B-cell non-Hodgkin's lymphoma (NHL). This indication includes patients with Rituxan (rituximab)-refractory follicular NHL. Zeva lin has been approved as part of a therapeutic regimen involving Rituxan.
Zeva lin consists of a monoclonal antibody linked to the radioactive isotope yttrium-90. After infusion into a patient, the monoclonal antibody targets the CD20 antigen, which is found on the surface of mature B cells and B-cell tumors. In this manner, cytotoxic radiation is delivered directly to malignant cells.
Clinical Results
Zeva lin received both a full approval and an accelerated approval based on results from two major US efficacy studies.
The study that supported the full approval of Zeva lin included 54 subjects.
The subjects were diagnosed with relapsed follicular lymphoma, and they no longer adequately responded to Rituxan treatment. An overall response rate of 74% was achieved with Zeva lin treatment, with 15% of subjects experiencing a complete response.
Accelerated approval of Zeva lin was supported by a randomized, controlled phase III trial.
The trial included 143 subjects with relapsed or refractory, low grade or follicular NHL or transformed B-cell NHL.
An overall response rate of 80% was obtained in subjects receiving the Zeva lin therapeutic regimen (73 subjects), compared to 56% for the subjects receiving Rituxan alone (70 subjects). Thirty percent of Zeva lin-treated subjects experienced a complete response, compared to a 16% complete response rate for Rituxan-treated
subjects.
Side Effects
In clinical trials, serious adverse reactions caused by the Zeva lin therapeutic regimen included infections, allergic reactions, and hemorrhage while thrombocytopenic. In addition, the development of myeloid malignancies and dysplasias have been reported.
Adverse events that occurred in greater than 5% of subjects include(but are not limited to) the following:
Nausea
Vomiting
Diarrhea
Anorexia
Thrombocytopenia (decreased number of blood platelets)Neutropenia (decreased number of white blood cells)
Anemia
Arthralgia (joint pain)
Dizziness
Dyspnea (difficult or labored breathing)
Increased cough
Mechanism of Action
The complementarity-determining regions of Ibritumomab bind to the CD20 antigen on B lymphocytes.
Ibritumomab, like Rituximab, induces apoptosis in CD20+ B-cell lines in vitro. The chelate tiuxetan, which tightly binds In-111 or Y-90, is covalently linked to the
amino groups of exposed lysines and arginines contained within the antibody.
The beta emission from Y-90 induces cellular damage by the formation of free radicals in the target and neighboring cells.
(from Zeva lin Prescribing Information)Additional Information
Schering AG has the marketing rights to Zeva lin outside of the United States.
For more information on Zeva lin, please visit IDEC Pharmaceuticals.
Additional information on non-Hodgkin's lymphoma can be obtained through the National Cancer Institute.