【商 品 名】Mylotarg 【通 用 名】gemtnzumab 【中 文 名】麦罗塔 【开发公司】惠氏、Wyeth CellTech ---------------------------------------------------------------------------- Gemtuzumab ozogamicin [别名] Mylotarg. [药理] 本品是一种抗体导向肿瘤药，由重组人源化lgG4单克隆抗体（吉妥珠单抗，hP67.6)与细胞毒抗肿瘤抗生素刺孢霉素（calicheamicin）健合而成。 本品与抗原CD33特异性结合后可被髓细胞“内在化”，在髓细胞的溶酶体内通过水解作用释放刺孢霉素．刺孢霉素与ＤＮＡ双链断裂，诱导细胞死亡。对急性髓西白血病（AMI)病人的原始细胞、单核细胞合HL-60细胞株的体外实验均显示，本品能诱导剂量依赖性凋亡。 成年CD33阳性的AML复发病人（n=58)单剂量静脉输注本品（9ml/m2）后，平均Cmax（最大血药浓度）为（2.86±1.35)mg/L,平均AUC (曲线下面积)为（123±105)mg/(L•h)，血浆清除半衰期为（72.4±42.0)小时。游离型刺孢霉素的Cmax为（0.079±0.093)mg/(L•h)，总刺孢霉素的平均AUC为（2.47±1.82) mg/(L•h)，血浆清除半衰期 为（45.1±25.2)小时。对药物动力学参数的统计分析表明，未见显著的性别差异和年龄差异。 [适应症] 用于急性粒细胞白血病（AML）的单药治疗，在60岁以上、CD33阳性，首次复发且不宜用其他药物化疗的病人。 [用法] 静脉输注：推荐剂量为9mg/m2采用外周静脉中心静脉或作静脉输注2小时，14天后重复给药1次，共给药2次。配制方法：待本品粉针达到室温时，加入5 ml注射用水，使成为1mg/ml的溶液，给药前取适量药液稀释于100ml生理盐水中，立即静脉输注。 为减少过敏反应和输注反应，每次给药前1小时口服对乙酰氨基酚（扑热息痛）0.5～1.0(1～2片)和苯海拉明40mg,肌注.必要时,间隔4小时后再次口服对乙酰氨基酚0.1～1.0g. [不良反应] 滴注结素后24h内可能出现急性输注反应,包括寒战、发热、恶心、呕吐、头痛、低血压、高血压、缺氧、呼吸困难和高血糖，用药后2～4小时内缓解。常见与首次给药，第2次给药后较少发生。 常见骨髓移植、肺浸润或水肿、乏力、腹泻、腹痛、高胆红素血症、肝转氨酶升高、感染、低钾血证、厌食、便秘、局部反应、皮疹、疼痛、外周水肿、失眠、头晕、背痛、咽炎、LDH升高、心动过速、鼻炎、低镁血症、抑郁、关节痛、口腔粘膜炎等。 [注意事项] 1． 已知对本品或其中任何成分过敏者、妊娠和哺乳妇女，禁用。 2． 本品不得静脉推注；应该使用带有低蛋白结合终端滤器的单独输液管路，不得与其他药物混合。 3． 应在有经验的医师指导下使用。用药期间应监测病人的电解质、肝功能、全血细胞计数和血小板计数。滴注时和滴注后4小时内密切监测生命体征。 4． 所有病人在推荐剂量下均会出现严重的骨髓抑制反应，表现为中性粒细胞减少症、血小板减少症和贫血。首次给药后平均40.5天恢复。 5． 哮喘、慢性阻塞性肺病（COPD）等呼吸系统疾病者发生肺浸润、肺水肿、肺功能不全、缺氧、急性呼吸窘迫综合征的危险性大。若患者出现肺水肿或急性呼吸窘迫综合征，应立即停药。 6． 肝功能不全者应慎用本品。临床研究中发现部分患者可出现高胆红素血症、血清ALT和AST升高。肝毒性严重者可出现肝功能衰竭。 7． 为防止发生肿瘤溶解综合症，使用本品前可考虑用羟基脲或白细胞除法使白细胞计数降至30×109/L以下。 8． 采用别嘌醇和水化作用等适当措施，防止发生高尿酸血症。 9． 若患者在治疗期间出现任何不适、或服用了任何处方药和OTC药物，应尽早告知医生。 10． 本品剂量高于9mg/m2时或与其他药物合用时的疗效和不良反应尚不清楚。 [制剂] 注射粉针剂。 [贮法] 避光、于2～8摄氏度下保存。药物溶解后，贮于冰箱中，最多存放8小时。 Mylotarg (Gemtuzumab Ozogamicin) Mylotarg (gemtuzumab ozogamicin) is a powerful treatment for the myeloid leukemia, used as a last resort in the patients older than 60, when any other medications are too risky for their lives or proven to be ineffective. The leukemia is a cancer of the blood cells, produced by the bone marrow. The bone marrow produces too many white cells, resulting in an abuse. They stop fulfilling their functions and keep multiplying, when the process should normally stop. At some point, they end up replacing most other cells in the blood. At that moment, the blood cannot deal with all the normal functions. The patients end up with a constant tiredness, can bleed and get hurt extremely easy and can catch infections or other diseases they would normally not. Basically, the immune system is destroyed. Mylotarg (gemtuzumab ozogamicin) is based on gemtuzumab. It interferes with the multiplication of these cells, preventing the disease evolution. The medication was FDA approved in 2000. It didn't manage to stay too much on the market. In 2010, the manufacturer – Pfizer – has decided to withdrawn it from all the markets due to multiple studies revealing no beneficial effects over the patients. However, some doctors may still use it in some countries. Administration Mylotarg (gemtuzumab ozogamicin) was given intravenously through an IV line. Due to the risky adverse reactions, the medicine could only be taken in a hospital or a clinic, under the strict monitoring of the specialist doctor. The infusion was supposed to be slow and needed at least 120 minutes to be over. Unlike other similar drugs, this was not the type of drug you could get at home. Contraindications The medication was contraindicated in the patients with allergies to gemtuzumab or any other ingredients. Other diseases that contraindicated this drug or at least required dosage adjustments include: Respiratory conditions Renal or hepatic dysfunctions Any infections