药品信息:
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.
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吉姆单抗/奥佐米星治疗急性白血病的基础与临床研究进展 刘兵(综述) 陈虎(审校) 军事医学科学院附属医院造血干细胞移植科,北京市100071 国际标准刊号:ISSN 1006-5725 国内统一刊号:CN 44-1193
摘要: 吉姆单抗/奥佐米星(GO)由人源化IgG4抗CD33单克隆抗体与细胞毒药物刺孢霉素的衍生物结合形成.为美国Wyeth公司生产。2000年5月美国食品及药品管理局(FDA)批准GO单药治疗年龄大于60岁的CD33阳性急性髓系白血病(AML)首次复发患者,缓解率约30%。GO的联合治疗方案进入临床试验后,也显示出良好的治疗效果.应用范围有所扩大。近年来GO的基础研究和临床研究互相促进,本文对此进行综述。[第一段] —— 全文请见本药内容附件 ----------------------------------------------
吉妥单抗(gemtuzumab ozogamicin/Mylotarg) 抗CD33 [别名]Mylotarg 、CMA676、GO
[来源] 重组人源化抗CD33单抗与细胞毒药物卡奇霉素的复合物。其中单抗为人鼠源氨基酸序列,与细胞毒抗肿瘤抗生素(卡奇霉素)偶联而成。
[作用机制] CD33表达于80%以上的急性髓性白血病(AML)患者白血病细胞上。本品静脉注射后,偶联屋中的抗体与复合物可被靶细胞胞饮。在细胞内,卡奇霉素从偶联物上水解游离,与DNA结合,使其双螺旋断列,导致细胞死亡。本品对表达CD33抗原的细胞毒性是不表达该抗原细胞的7万余倍。另外,由于造血干细胞不受药物治疗的影响,因而骨髓抑制较轻。作为一线药物治疗老年AML和高危MDS,Mylotarg 单药疗效不及化疗。目前正在进行Mylotarg 与氟达拉滨+阿糖胞苷、拓扑替康+阿糖胞苷和IL-11联合用药的临床研究。
[药动学] 首次推荐剂量9mg/m2,静脉点滴持续2小时,半衰期45小时。第二次予以9mg/m2,半衰期延长至60小时,曲线下面积也比初次用药后增加一倍。
[适应症] 首次复发的60岁以上CD33抗原阳性的急性髓细胞性白血病或不宜用细胞毒性药物治疗的CD33阳性的AML患者。
[不良反应]
- 全身反应:腹痛、乏力、背痛、寒战、发热、头痛、败血症、肿瘤溶解综合征。
- 循环系统:低血压、高血压、心律失常。
- 消化系统:食欲不振、恶心、呕吐、便秘、腹泻、腹胀、消化不良、胃炎、肝毒性、肝静脉血栓。
- 血液系统;骨髓抑制(较严重)、贫血、血小板减少、出血(鼻出血、脑出血、瘀斑、颅内出血、血尿、阴道出血)、弥漫性血管内凝血。
- 代谢系统:低钾血症、低镁血症、乳酸脱氢酶升高、高血糖。
- 肌肉骨骼:关节痛。
- 神经系统:抑郁、失眠、眩晕。
- 呼吸系统:呼吸困难、低氧血症、肺炎、咳嗽加重、咽炎、鼻炎。
- 皮肤及附属物:单纯疱疹、皮疹、局部反应、周围水肿。
[禁忌症] 禁用于对本品或者本品中其他组成成分过敏的患者。
[规格] 针剂,4.5mg;冻干粉剂。
[开发公司]:Pfizert
------------------------------------ 详细处方信息请见本药内容附件PDF文件(2020112501370010.pdf)的“原文Priscribing Information” ------------------------------------
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