英文药名：RASURITEK（Rasburicase（Genetical Recombination））

中文药名：拉布立酶重组注射剂

生产厂家：赛诺菲有限公司

ラスリテック点滴静注用1.5mg／ラスリテック点滴静注用7.5mg

药物分类名称
尿酸降解酶制剂用于癌症化疗
批准日期：2010年4月
商標名
RASURITEK
一般名
ラスブリカーゼ（遺伝子組換え）
Rasburicase（Genetical Recombination）
本　質
由表达来自黄曲霉菌的尿酸氧化酶cDNA重组产生的301个氨基酸残基（C 1523 H 2383 N 417 O 462 S 7;分子量34,151.19）氨基末端乙酰化的相同亚基的四聚体蛋白质。
药效药理
该药剂将尿酸氧化分解成尿囊素和过氧化氢，从而降低血尿酸水平。
适应病症
与癌症化疗相关的高尿酸血症
用法与用量
通常在30分钟内每天一次静脉滴注0.2mg/kg作为速释肽。 管理期限最长为7天。
临床结果
[国内临床试验]
白血病或恶性淋巴瘤成年患者，剂量为0.15mg/kg时，为0.2mg/kg的给予每只25箱子研究中，100％的有效率为96％1）。
在造血肿瘤儿科患者的研究中，剂量为0.15mg/kg时，为0.2mg/kg的给药于各15例，分别有效93.3％100％2）。
有效的例子的定义如下所示。
开始后到达，并在最后一次给药（第5天）48小时（6.5毫克/升：：7.5毫克/分升13岁的患者的下超过13岁的患者）后血浆尿酸水平端点直到拉布立酶初始给药开始维护案例长达24小时
（注）该药的批准单次剂量为0.2 mg/kg。
[海外临床试验]
在别嘌呤醇作为对照的III期比较研究（所有患有白血病或恶性淋巴瘤的儿童）中，将该产品给予27名患者，并将别嘌呤醇给予25名患者。施用后尿酸AUC长达96小时（平均值±SD）的比较的结果，这种药物组为128±70毫克·H /dL的，比329±129mg显著低·H / dL的别嘌呤醇给药组（单因素方差分析，p <0.0001）。在该研究中，别嘌呤醇以每剂25-210mg（中位数100mg）的剂量给药，平均6.3天的15.5倍给药。
包装规格
静脉滴注
1.5mg×3小瓶（附有溶解液）

7.5毫克×1小瓶（附带静脉滴注）

制造业销售
赛诺菲有限公司
提示；以上中文资料不够完整，使用者以原处方为准。
完整说明书附件：http://www.info.pmda.go.jp/go/pack/3959415F1025_1_04/3959415F1025_1_04?view=body
Common name: Ras Blocase (genetical recombination) "Rasulitec ® for intravenous infusion 1.5 mg, same 7.5 mg"
Laslitec ® (generic name rasburicase [genetical recombination]) is the only uricolytic enzyme drug that has indication for hyperuricemia, which is a typical pathology of oncolytic syndrome (TLS). Until now, for hyperuricemia associated with TLS, infusion (increase urine volume and promote excretion of uric acid), alkalization of urine (accelerate excretion by increasing uric acid solubility in urine), allopurinol ( Uric acid synthesis inhibitor) was used to control plasma uric acid level, but in either case there was a problem that it took time to lower the uric acid level and could not cope with a rapid increase in uric acid value.
Since Raslitec ® is an enzyme preparation that directly degrades uric acid, it is a drug that can reliably expect a lower uric acid lowering effect in a short time compared to conventional treatments, and an approach to hyperuricemia accompanying TLS in the future It is expected as a drug that greatly changes.
Name of drug classification
Uric Acid Degradation Enzyme Preparation for Cancer Chemotherapy
Sales name
Raslitec intravenous drip infusion for 1.5 mg
common name
Ras Blicase (genetical recombination)
Rasburicase (Genetical Recombination)
Essence
A tetramer of the same subunit consisting of 301 amino acid residues (C 1523 H 2383 N 417 O 462 S 7; molecular weight: 34, 151.19) amino-terminal acetylated recombinantly produced by expression of urate oxidase cDNA derived from Aspergillus flavus Protein
composition
Active ingredient: raspuricase (genetical recombination)
Vial (3 mL container): 1.5 mg
Additive: D-mannitol
Vial (3 mL container): 10.6 mg
Additive: L-alanine
Vial (3 mL container): 15.9 mg
Additive: sodium hydrogen phosphate hydrate
Vial (3 mL container): 12.6 - 14.3 mg
Attached lysis solution
Additives: polyoxyethylene (160) polyoxypropylene (30) glycol
Ampoule (2 mL container): 1.0 mg contained in 1.0 mL ampule
Contraindication
Patients with a history of hypersensitivity to the ingredients of this drug
Patients with deficiency in glucose-6-phosphate dehydrogenase (G6PD) or other erythrocyte enzyme abnormalities known to cause hemolytic anemia [May cause hemolytic anemia. [Warning] and "3. Side effects (1) Serious side effects"]
Indication or effect
Hyperuricemia associated with cancer chemotherapy
When administering this drug, select an indication patient in consideration of the onset risk of oncolytic syndrome, and administer it only when it is considered that management of blood uric acid value is insufficient in existing supportive therapy.
The efficacy and safety of this drug in the treatment of hyperuricemia developed after cancer chemotherapy has not been established[There is no use experience]
Usually, intravenous drip infusion of 0.2mg/kg as a raspuricase once a day over 30 minutes. The administration period should be a maximum of 7 days.
This drug should be administered 4 to 24 hours before starting cancer chemotherapy.
Effectiveness and safety when the administration period exceeds 7 days have not been established. [There is no use experience]
Monitor clinical symptoms and blood uric acid concentration and keep administration of this drug in a minimum period necessary for management of blood uric acid concentration.
The efficacy and safety of this product once established after the first use of this product (administration for up to 7 days) has not been established. [Less experience in using. Refer to "2. Important basic attention" section]
Preparation of injection solution
Dissolve 1 vial of this product in 1 ampoule of attached lysis solution and dilute the necessary amount with 50 mL of physiological saline. For patients whose age is 24 months or less, the physiological saline used for dilution of this drug can be reduced to 10 mL. When dissolving this drug, dissolve gently so as not to foam. Mix immediately with physiological saline after dissolution. [See "9. Application note"]
Careful Administration
Patients with an allergy-prone constitution [There is a danger of severe immediate allergic reactions appearing]
Serious side effects
Shock, anaphylactoid symptoms (Frequency unknown)
Severe hypersensitivity including anaphylactic shock may occur, so if such symptoms are observed, administration of this drug should be immediately stopped and appropriate measures should be taken.
Hemolytic anemia (Frequency unknown)
Hemolytic anemia may occur, so observe the condition of the patient adequately, if anemic symptoms are observed stop administration of this drug immediately and take appropriate measures.
Methemoglobinemia (Frequency unknown)
Since methemoglobinemia may occur, if symptoms such as cyanosis are observed, administration of this drug should be immediately stopped and appropriate measures should be taken.
Medicinal pharmacology
This agent oxidizes uric acid and decomposes into allantoin and hydrogen peroxide, thereby lowering blood uric acid level.