近日，美国FDA已批准其Arranon（nelarabine）注射剂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（T-ALL）和T细胞淋巴瘤（T-LBL）患者。
奈拉滨(Nekarabine，美国上市的商品名：Arranon，欧洲上市的商品名：Atriance 公司：葛兰素史克)是一种嘌呤类似物抗代谢药，其批准上市日期为2005年10月28日。
ARRANON（奈拉滨 nelarabine）注射液
美国初步批准：2005年
警告：
神经不良反应请参阅完整的处方信息，以获得完整的盒装警告。
使用ARRANON已经报道了严重的神经性不良反应。这些不良反应包括改变的精神状态，包括严重的嗜睡，中枢神经系统的影响，包括抽搐，以及周围神经病变，从麻木和感觉异常到运动性虚弱和瘫痪。还有报道称，与脱髓鞘有关的不良反应和在外观上与吉兰-巴利综合征相似的上行性周围神经病。
从ARRANON停止治疗后，这些不良反应的完全恢复并不总是发生。强烈建议严格监测神经性不良反应，并且应该停止ARRANON用于NCI常见毒性标准2级或更高的神经性不良反应。
作用机制
奈拉滨是脱氧鸟苷类似物9-β-D-阿拉伯呋喃糖基鸟嘌呤（ara-G）的前药，核苷代谢抑制剂。 奈拉滨通过腺苷脱氨酶（ADA）脱甲基化为ara-G，被脱氧鸟苷激酶和脱氧胞苷激酶单磷酸化，随后转化为活性5'-三磷酸，ara-GTP。 ara-GTP在白血病母细胞中的积累允许并入脱氧核糖核酸（DNA），导致DNA合成和细胞死亡的抑制。 其他机制可能有助于奈拉滨的细胞毒性和全身毒性。
适应症和用法
ARRANON是一种核苷代谢抑制剂，用于治疗患有T细胞急性淋巴细胞白血病和T细胞淋巴细胞淋巴瘤的患者，其疾病在用至少两种化疗方案治疗后没有反应或复发。这种使用是基于完全反应的诱导。还没有进行展示增加的存活或其他临床益处的随机试验。
剂量和给药
•成人剂量：1,500mg/m²，在第1,3和5天，每21天静脉注射2小时。
•儿科剂量：650mg/m²，每天1小时静脉注射，连续5天，每21天重复一次。
•停止治疗≥Grade2神经系统反应。
•剂量可能会延迟血液学反应
•采取措施预防高尿酸血症。
剂量形式和强度
250mg/50mL（5mg/mL）小瓶
禁忌症
没有。
警告和注意事项
•已报道了严重的神经反应。监测神经毒性的体征和症状。
•血液反应：应定期监测全血细胞计数，包括血小板。
•如果给予孕妇，可能会发生胎儿伤害。建议妇女在服用ARRANON时不要怀孕。
不良反应
最常见的（≥20％）不良反应为：
•成人：贫血，血小板减少，中性粒细胞减少，恶心，腹泻，呕吐，便秘，疲劳，发热，咳嗽和呼吸困难
•儿科：贫血，中性粒细胞减少，血小板减少症和白细胞减少
最常见的（> 10％）神经不良反应是：
•成人：嗜睡，头晕，外周神经系统疾病，感觉迟钝，头痛和感觉异常
•儿科：头痛和外周神经系统疾病
药物相互作用
不推荐与腺苷脱氨酶抑制剂（例如喷司他丁）组合施用。
在特定人群中使用
•肾损伤：严密监测中度或重度肾损伤患者的毒性。
•肝损害：严重监测严重肝损害患者的毒性。
临床试验结果：
Arranon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，Arranon治疗的总体中位生存时间为成年人21周、儿童13周。
完整资料附件：
1）:https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=893c95d7-d9b6-4064-db97-91dd21ce7e40
2）:https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=fffa5d75-0dba-4ad7-a252-5f60fa28489a

Arranon Injection approved by US FDA
New option for children and adults with treatment resistant T-cell acute lymphoblastic leukemia (T-ALL) and T-cell lymphoblastic lymphoma (T-LBL)
 U.S. Food and Drug Administration (FDA) has approved ARRANON® (nelarabine) Injection, a chemotherapy agent, for the treatment of patients with T-cell acute lymphoblastic leukemia (T-ALL) and T-cell lymphoblastic lymphoma (T-LBL) whose disease has not responded to or has relapsed following treatment with at least two chemotherapy regimens. This use is based on the induction of complete responses. Randomized trials demonstrating increased survival or other clinical benefit have not been conducted.
Approximately 1,600 adults and children are diagnosed with T-ALL or T-LBL in the U.S. each year. A subset of these patients will relapse or develop disease that is refractory to treatment. There is no standard of treatment for these patients and their prognosis is particularly poor. To facilitate the development of ARRANON for this relatively small group of patients, GSK worked closely with the National Cancer Institute (NCI) of the National Institutes of Health (NIH), the Children's Oncology Group (COG) and the Cancer and Leukemia Group B (CALGB), in conjunction with the Southwest Oncology Group (SWOG).
"ARRANON affirms GSK's long-term commitment to discover drugs for the treatment of cancer and to working with others in the cancer community to develop treatments for even the most difficult to treat malignancies," said Paolo Paoletti, M.D., Senior Vice President of the Oncology Medicine Development Center, at GSK. "We are proud to meet this critical need and will continue to work closely with the oncology community to evolve the treatment paradigm."
ARRANON received accelerated approval, granted by the FDA to medicines for treating serious or life-threatening illnesses that address an unmet medical need, based on complete response rates demonstrated in two Phase II trials in patients who had exhausted standard treatment options. Post-marketing evaluation to verify and describe the product's clinical benefit will be pursued through a randomized, multi-center Phase III trial that will be conducted by COG and sponsored by the NCI under a Clinical Trials Agreement with GSK. The Phase III study will assess both event-free survival at four years and minimal residual disease in the post-consolidation phase for patients receiving standard therapy with or without nelarabine.
"ARRANON represents new hope for adults and children suffering from these rare and deadly cancers," said Kevin Lokay, Vice President of Oncology and Acute Care at GSK. "As the first in a series of innovative medicines set to emerge from GSK's robust oncology pipeline over the next few years, ARRANON is an important milestone for our oncology business and provides a glimpse of our promise for the future."
More than 980 patients have received ARRANON as part of clinical trial protocols to date. The two multi-center pivotal Phase II clinical trials included a total of 39 adults and 151 children with T-ALL or T-LBL. These studies were conducted by cooperative groups under the auspices of the NCI. The primary efficacy results were based on 28 adults and 39 children that had multiple relapses following, or were refractory to, at least two prior induction regimens. In these groups, a total of 21 percent of the adults and 23 percent of the children achieved a complete response (CR) or a complete response without full hematological recovery (CR*) with single agent ARRANON. Remissions were generally long enough to allow for stem cell transplant procedure, often the intent following successful induction of remission. Following Arranon, patients had a median overall survival of 21 weeks for adults and 13 weeks for children.
In clinical studies of ARRANON, hematologic toxicity was the most common Grade 3 (moderate) or 4 (severe) adverse event. Consistent with various other cytotoxic agents, ARRANON is associated with neurological events, some considered severe. Close monitoring for neurologic events is strongly recommended and dosing of ARRANON should be discontinued for neurologic events of Grade 2 or greater.
About ARRANON
ARRANON was discovered by GSK scientists under the direction of Thomas Krenitsky, Ph.D. The early work, continued support and involvement of Gertrude Elion, Nobel Laureate for Medicine in 1988, is recognized as an important factor in the development of ARRANON.
ARRANON is a water-soluble prodrug of ara-G, a T-cell selective nucleoside analog. Accumulation of the active form of ARRANON (ara-GTP) in cancer cells leads to inhibition of DNA synthesis, resulting in cell death. ARRANON is toxic to T-cells with much greater potency and specificity than other types of white blood cells (B-cells, monocytes/macrophages).

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产地国家：美国
原产地英文商品名:
Arranon 250mg/50mL（5mg/mL）/VIAL 6VIALS/BOX 
原产地英文药品名:
nelarabine
中文参考商品译名:
阿仑恩注射剂 250毫克/50毫升（5毫克/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:
葛兰素史克
生产厂家英文名:
GlaxoSmithKline
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产地国家：美国
原产地英文商品名:
ARRANON 250mg/50mL（5mg/mL）/VIAL 6VIALS/BOX 
原产地英文药品名:
NELARABINE
中文参考商品译名:
ARRANON注射剂 250毫克/50毫升（5毫克/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:
诺华制药
生产厂家英文名:
NOVARTIS PHARMACEUTICALS
NDC: 00007-4401-06
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产地国家：美国
原产地英文商品名:
ARRANON 250mg/50mL（5mg/mL）/VIAL 6VIALS/BOX 
原产地英文药品名:
NELARABINE
中文参考商品译名:
ARRANON注射剂 250毫克/50毫升（5毫克/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:
诺华制药
生产厂家英文名:
NOVARTIS PHARMACEUTICALS
NDC: 00078-0683-06