英文药名：MYLOTARG Injection(Gemtuzumab Ozogamicin[Genetical Recombination]) 中文药名：吉妥珠单抗奥佐米星重组冻干粉注射剂 生产厂家：辉瑞公司日本 マイロターグ点滴静注用5mg Mylotarg(Gemtuzumab Ozogamicin,CMA-676)是人源化抗CD33单克隆抗体与抗肿瘤抗生素Calicheamicin偶联而成的一个新的抗体导向化疗药药 治疗类别名称 抗肿瘤药 抗肿瘤抗生素结合的抗CD33单克隆抗体 批准日期：2008年6月 开发商：惠氏 商標名 MYLOTARG Injection 5mg 一般名 ゲムツズマブオゾガマイシン（遺伝子組換え） Gemtuzumab Ozogamicin（Genetical Recombination） 化学名 Immunoglobulin G4（human-mouse monoclonal hP67.6 γ4-chain anti-human antigen CD33）, disulfide with human-mouse monoclonal hP67.6κ-chain, dimer, conjugate with methyl（1R,4Z,8S,13E）-13-［2-［［2-［［［p-（3-carbamoylpropoxy）-α-methylbenzylidene］hydrazino］carbonyl］-1,1-dimethylethyl］dithio］ethylidene］-8-［［4,6-dideoxy-4-［［［2,6-dideoxy-4-S-［4-［（6-deoxy-3-O-methyl-α-L-mannopyranosyl）oxy］-3-iodo-5,6-dimethoxy-o-toluoyl］-4-thio-β-D-ribo-hexopyranosyl］oxy］amino］-2-O-［2,4-dideoxy-4-（N-ethylacetamido）-3-O-methyl-α-L-threo-pentopyranosyl］-β-D-glucopyranosyl］oxy］-1-hydroxy-11-oxobicyclo［7.3.1］trideca-4,9-diene-2,6-diyne-10-carbamate 構造式 本質 小鼠通过从人免疫球蛋白G4恒定区（κ链和γ4链）的cDNA的表达和可变结构域框架序列和人源化鼠抗CD33单克隆抗体，包括鼠抗CD33单克隆抗体的互补决定区的骨髓瘤细胞（NS0细胞）组成的糖蛋白中产生1322个氨基酸残基（分子量：约150,000）和棘孢SSP缀合物从Calichensis细菌和分离的细胞毒性抗肿瘤抗生素卡奇霉素。 （分子量：约153000） 条件批准 试用情况在日本是非常有限的，另外，在临床试验中感染，出血，由于严重的副作用，如肝功能不全的发生已经观察到，商业之后，按照一定的数量的情况下的数据还有，直到它被集成，通过实现使用效果调查登记的所有情况下，要把握这种药物的使用患者的背景资料收集安全性和有效性，药物的适当性数据采取必要的措施来使用。 组成 在1瓶： 有效成分 吉妥珠单抗奥佐米星（基因重组）5mg 药效药理 1. 抗肿瘤作用 (1) 体外试验 针对CD33阳性人急性早幼粒细胞性白血病HL-60细胞，细胞毒活性已经观察到。此外，NOMO-1是表达CD33，NB4，NKM-1细胞杀伤活性的细胞对已观察到其他人白血病细胞。 (2) 体内试验 HL-60细胞显示出抗肿瘤作用通过静脉内施用在异种移植模型中皮下植入裸鼠中。 2. 作用机序 在该药物的加利车霉素的抗肿瘤剂缀合衍生物是抗肿瘤抗生素和人源化抗CD33抗体hP67.6，被掺入到细胞中后结合表达CD33抗原的白血病细胞示出了抗肿瘤效果发挥所释放的卡奇霉素衍生物的细胞杀伤活性。 顺便提及，在重复剂量在大鼠和食蟹猴中不表达CD33抗原，认为毒性研究来源于卡奇霉素衍生物的细胞毒性是由于吉妥单抗奥佐米星毒性的非特异性摄取目前有报道。 适应病症 急性髓性白血病复发性或难治性CD33阳性 用法与用量 成人，吉妥珠单抗单抗臭氧（为蛋白质量）蛾霉素1个剂量9毫克/米2，用2小时静脉内施用输注。施用的频率，以至少14天，2次的给药间隔。 包装规格 静脉内输注[冻干粉剂] 5mg：1瓶 生产和销售 辉瑞公司日本 完整资料附件：http://www.info.pmda.go.jp/go/pack/4239400D1030_2_05/ 特别提醒：Mylotarg目前在全球全部下架（除日本医药内有货），如市面上的货全部为假货，敬请采购买者认清，谨防上当！！ Product Overview MYLOTARG(gemtuzumab ozogamicin for Injection) Indication and Usage MYLOTARG is indicated for the treatment of patients with CD33+ acute myeloid leukemia in first relapse who are 60 years of age or older and who are not considered candidates for other cytotoxic chemotherapy. The safety and efficacy of MYLOTARG in patients with poor performance status and organ dysfunction has not been established. The effectiveness of MYLOTARG is based on overall response rates. There are no controlled trials demonstrating a clinical benefit, such as improvement in disease-related symptoms or increased survival, compared to any other treatment.   Important Safety Information  WARNINGS: MYLOTARG should be administered under the supervision of physicians experienced in the treatment of acute leukemia and in facilities equipped to monitor and treat leukemia patients. There are no controlled trials demonstrating efficacy and safety using MYLOTARG in combination with other chemotherapeutic agents. Therefore, MYLOTARG should only be used as single agent chemotherapy and not in combination chemotherapy regimens outside clinical trials. Severe myelosuppression occurs when MYLOTARG is used at recommended doses. HYPERSENSITIVITY REACTIONS INCLUDING ANAPHYLAXIS, INFUSION REACTIONS, PULMONARY EVENTS: MYLOTARG administration can result in severe hypersensitivity reactions (including anaphylaxis), and other infusion-related reactions which may include severe pulmonary events. Infrequently, hypersensitivity reactions and pulmonary events have been fatal. In most cases, infusion-related symptoms occurred during the infusion or within 24 hours of administration of MYLOTARG and resolved. MYLOTARG infusion should be interrupted for patients experiencing dyspnea or clinically significant hypotension. Patients should be monitored until signs and symptoms completely resolve. Discontinuation of MYLOTARG treatment should be strongly considered for patients who develop anaphylaxis, pulmonary edema, or acute respiratory distress syndrome. Since patients with high peripheral blast counts may be at greater risk for pulmonary events and tumor lysis syndrome, physicians should consider leukoreduction with hydroxyurea or leukapheresis to reduce the peripheral white count to below 30,000/µL prior to administration of MYLOTARG. (See WARNINGS) HEPATOTOXICITY: Hepatotoxicity, including severe hepatic veno-occlusive disease (VOD), has been reported in association with the use of MYLOTARG as a single agent, as part of a combination chemotherapy regimen, and in patients without a history of liver disease or hematopoietic stem-cell transplant (HSCT). Patients who receive MYLOTARG either before or after HSCT, patients with underlying hepatic disease or abnormal liver function, and patients receiving MYLOTARG in combinations with other chemotherapy are at increased risk for developing VOD, including severe VOD. Death from liver failure and from VOD has been reported in patients who received MYLOTARG. Physicians should monitor their patients carefully for symptoms of hepatotoxicity, particularly VOD. These symptoms can include: rapid weight gain, right upper quadrant pain, hepatomegaly, ascites, elevations in bilirubin and/or liver enzymes. However, careful monitoring may not identify all patients at risk or prevent the complications of hepatotoxicity. (See WARNINGS and ADVERSE REACTIONS sections.) MYLOTARG is contraindicated in patients with a known hypersensitivity to gemtuzumab ozogamicin or any of its components and in lactating mothers. MYLOTARG may cause fetal harm when administered to a pregnant woman. The reported rate of Grade 3 or 4 thrombocytopenia, neutropenia, anemia, and bleeding were 99%, 98%, 52%, and 13%, respectively. Thirty percent of patients experienced severe infections, including sepsis (17%) and pneumonia (8%). The most common adverse events (≥20%) were fever (82%), nausea (68%), chills (66%), vomiting (58%), thrombocytopenia (50%), leukopenia (47%), headache (37%), asthenia (36%), abdominal pain (32%), diarrhea (32%), epistaxis (28%), dyspnea (26%), hypokalemia (26%), sepsis (26%), anorexia (25%), stomatitis (25%), liver function tests abnormal (24%), constipation (23%), anemia (22%), local reaction (22%), herpes simplex (21%), and hypotension (20%). MYLOTARG can produce a postinfusion symptom complex of fever and chills, and less commonly hypotension and dyspnea during the first 24 hours after administration. Patients should receive diphenhydramine 50 mg po and acetaminophen 650-1000 mg po 1 hour before MYLOTARG administration. Two additional doses of acetaminophen 650-1000 mg po every 4 hours may be given. Fever and chills were commonly reported despite premedication with diphenhydramine and acetaminophen. Vital signs should be monitored during infusion and for 4 hours following infusion. Methylprednisolone given prior to MYLOTARG infusion may ameliorate infusion-related symptoms. Severe myelosuppression will occur in all patients given the recommended dose of this agent. Careful hematologic monitoring is required. Systemic infections should be treated.