奈拉滨（Arranon）治疗T-ALL和T-LBIL
——用于T-细胞急性成淋巴细胞白血病(T-ALL)和T-细胞成淋巴细胞淋巴瘤(T-LBIL)
英文名称：Nekarabine
商品名称：Arranon
化学名称：9beta-D-Arabinofuranosyl-6-methoxy-9H-purin-2-amine
分子式：C11H15N5O5
分子量：297.27
CAS.NO：121032-29-9
剂   型：
原料药、注射液
适 应 症：
用于至少接受过两种化学疗法之后病情复发或对药物无应答的T细胞急性成淋巴细胞性白血病和T细胞淋巴瘤患者。
用法用量：
成人推荐剂量1500 mg/m²，静脉输注2小时，21天为一疗程，在第1、3、5天给药，无需稀释。儿童推荐剂量为650mg/m²，静脉输注1小时，21天为一疗程，连续输注5天，无需稀释。
质量标准：美国药典标准。
产品优势
2005年10月28日FDA快速通道批准葛兰素史克公司的奈拉滨在美国上市。其为脱氧鸟苷类似物9-β-阿糖鸟嘌呤(ara-G)的前药，ara-G水溶性差，加甲氧基为本药，在体内它被腺苷脱胺酶催化，脱甲氧基成为ara-G，经脱氧鸟苷激酶和脱氧胞嘧啶核苷激酶依次单磷酸化生成活性的5’-三磷酸ara-GTP，白血病母细胞中蓄积ara-GTP，PNP缺乏导致dGTP选择性地在T细胞中积累，而dGTP在B细胞中迅速降解，使其在B细胞中无堆积。细胞内dGTP的堆积可抑制DNA合成，阿糖鸟苷可选择性地毒杀T细胞白血病的细胞，导致细胞死亡。其他作用机制可能为奈拉滨的细胞毒性和系统毒性。
本药单药抗T细胞淋巴瘤较强，血液毒性低。T细胞急性淋巴细胞性白血病通常发病于较大的儿童、青少年和青年，较B细胞急性淋巴细胞性白血病不太常见。T细胞急性淋巴细胞性白血病和T细胞淋巴母细胞性淋巴瘤认为是同样疾病的不同临床表现，通常用长春新碱、强的松、蒽环类抗生素、天冬酰胺酶、环磷酰胺和阿糖胞苷治疗，通常预后复发。
临床应用
本项目主要用于治疗至少两种治疗方案无效或治疗后复发的T细胞急性淋巴细胞性白血病(T-ALL)和T细胞淋巴母细胞性淋巴瘤(T-LBL)。成人推荐剂量1500 mg/m²，静脉输注2小时，21天为一疗程，在第1、3、5天给药，无需稀释。儿童推荐剂量为650mg/m²，静脉输注1小时，21天为一疗程，连续输注5天，无需稀释。成人儿童的推荐治疗期未明确，临床试验中，除非患者病情加重，不能耐受毒性，即将进行骨髓移植或不再进行治疗。
临床评价
奈拉滨治疗后复发或治疗抵抗患者的多中心II期临床试验(28例成人患者，39例儿童患者)的数据显示，21%的成人和23%的儿童可获得完全缓解或未达到血液学完全复原的完全缓解。缓解的时间通常足够进行干细胞移植程序，奈拉滨治疗的总体中位生存时间为成年人21周、儿童13周。
本品主要的副作用是在神经方面，使用后一周左右开始会有经常性的疲累、想睡觉及头痛的状况，使用量越高状况也越明显，而且状况不会因为停药而完全改善，严重的情况会昏迷甚至产生癫痫需格外小心，但通常是在过量使用的情况下；其它常见的为血液方面副作用包括，贫血，嗜中性白血球与血小板数量降低，所以会增加因感染而发烧的危险性，所以必须固定作血液检查，给予必要的协助。
Important Safety Information
ARRANON(nelarabine) Injection should be administered under the supervision of a physician experienced in the use of cancer chemotherapeutic agents.
This product is for intravenous use only.
Neurologic Events: Severe neurologic events have been reported with the use of ARRANON. These events have included altered mental states
including severe somnolence, central nervous system effects including convulsions, and peripheral neuropathy ranging from numbness and paresthesias to motor weakness and paralysis.
There have also been reports of events associated with demyelination, and ascending peripheral neuropathies similar in appearance to Guillain-Barré syndrome.
Full recovery from these events has not always occurred with cessation of therapy with ARRANON. Close monitoring for neurologic events is strongly recommended, and ARRANON should be discontinued for neurologic events of NCI Common Toxicity Criteria grade 2 or greater.
In clinical studies of ARRANON, hematologic toxicity was the most common grade 3 (moderate) or 4 (severe) adverse event. Hematologic toxicity included neutropenia, thrombocytopenia, anemia, febrile neutropenia, or neutropenia with infection.
Other common toxicities included laboratory abnormalities including increased transaminases, gastrointestinal toxicity, fatigue, and asthenia.
Patients treated previously or concurrently with intrathecal chemotherapy or previously with craniospinal irradiation may be at increased risk for neurologic adverse events.
Women of child-bearing potential should be advised to avoid becoming pregnant while receiving treatment with ARRANON.
Appropriate measures (e.g., hydration, urine alkalinization, and prophylaxis with allopurinol) must be taken to prevent hyperuricemia of tumor lysis syndrome.
Nursing should be discontinued in women who are receiving therapy with ARRANON.
Because the risk of adverse reactions to this drug may be greater in patients with severe renal impairment (CLcr <30 mL/min), these patients should be closely monitored for toxicities when treated with ARRANON.
Because the risk of adverse reactions to this drug may be greater in patients with severe hepatic impairment (bilirubin >3.0 mg/dL),
these patients should be closely monitored for toxicities when treated with ARRANON.
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产地国家: 美国
原产地英文商品名:
ARRANON 5MG/ML 250MG/50ML/VIAL 6VIALS/BOX
原产地英文药品名:
NELARABINE
中文参考商品译名:
阿仑恩 5毫克/毫升 250毫克/50毫升/瓶 6瓶/盒
中文参考药品译名:
奈拉滨
生产厂家中文参考译名:
史克必成
生产厂家英文名:
SMITHKLINE BEECHAM
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产地国家: 葛兰素[日本公司]
原产地英文商品名:
ARRANON（アラノンジー静注用）250MG/50ML/VIAL 1VIALS/BOX
原产地英文药品名:
NELARABINE
中文参考商品译名:
阿仑恩（アラノンジー静注用）250毫克/50毫升/瓶 1瓶/盒
中文参考药品译名:
奈拉滨
生产厂家中文参考译名:
葛兰素
生产厂家英文名:
gsk
日文原资料附件：http://www.info.pmda.go.jp/go/pack/4229402A1028_1_04/