---------------------------------------------------------------
 详细处方信息以本药内容附件PDF文件（20096622583312.pdf）的“美国原文Priscribing Information”为准
---------------------------------------------------------------

部分中文奈拉滨处方资料（仅供参考）

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)
奈拉滨(Nekarabine，商品名：Arranon，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。

【适应症】
奈拉滨主要用于曾经接受过至少两种化疗方案治疗但仍无应答，或病情出现复发的急性T细胞型淋巴母细胞白血病及T细胞型淋巴母细胞淋巴瘤患者。

【药理及药代动力学】
奈拉滨是脱氧鸟苷类似物9-b-D-阿糖呋喃糖鸟嘌呤(ara-G)的前体药物。奈拉滨在腺苷脱氨酶(ADA)的作用下脱去甲基转变为ara-G，随后，又在脱氧鸟苷激酶和脱氧胞苷激酶的作用下，经单磷酸化作用途径转变为具有活性的ara-G三磷酸盐(ara-GTP)。ara-GTP可在白血病原始细胞中逐渐积聚，并与DNA相结合，从而起到抑制DNA合成，促进白血病细胞死亡的作用。此外，奈拉滨的抗癌机制可能还与其细胞毒性和全身毒性作用有关。

复发性白血病或淋巴瘤患者的药代动力学研究发现，奈拉滨和ara-G在血浆中的消除迅速，在给予1500mg/m2剂量的奈拉滨后，两者半衰期分别为30分钟和3小时。研究还发现，ara-G通常在奈拉滨给药完毕时达到峰浓度，而且其峰浓度数值通常也大于奈拉滨的峰浓度，表明奈拉滨可在体内迅速、完全地转化为ara-G。奈拉滨和ara-G部分经肾脏消除，28名成年患者在给予奈拉滨后24小时测得的奈拉滨和ara-G的平均肾排泄率分别为6.6±4.7%和27±15%。

【注意事项】
奈拉滨所致的神经毒性属于剂量限制性毒性反应。患者在用药期间应密切留意是否出现意识模糊、嗜睡、惊厥、共济失调、感觉异常和感觉减退等症状。曾经接受过鞘内化疗或颅脊放疗的患者应用奈拉滨后出现神经毒性反应的风险将增大。

奈拉滨还有可能引起白细胞减少症、血小板减少症、贫血和中性粒细胞减少症(包括发热性中性粒细胞减少症)，因此应用奈拉滨的患者应常规进行全血细胞计数(包括血小板计数)。

根据标准治疗方案，正在应用奈拉滨的肿瘤溶解综合征患者并发高尿酸血症时，可通过静脉水合方式加以缓解；存在高尿酸血症风险的患者还可考虑服用别嘌醇进行治疗。应用奈拉滨的免疫缺陷患者应避免注射活疫苗。

【药物相互作用】
迄今尚未见有关奈拉滨和ara-G药物相互作用的报道。体内实验发现，奈拉滨和ara-G不会明显抑制人细胞色素P450同功酶1A2、2A6、2B6、2C8、2C9、2C19、2D6或3A4的活性。

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.