部份中文喷司他汀处方资料（仅供参考） 【中文品名】喷司他汀 【药效类别】抗肿瘤药>抗代谢剂 【通用药名】PENTOSTATIN 【别　　名】Coforin, YK-176 【化学名称】Imidazo[4,5-d][1,3]diazepin-8-ol, 3-(2-deoxy-β-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydro-, (R)- 【CA登记号】[53910-25-1] 【结 构 式】 【分 子 式】C11H16N4O4 【分 子 量】268.27 【收录药典】 【开发单位】Yamasa Corporation 【首次上市】1996年，日本 【性　　状】 【用　　途】腺嘌呤脱氨酶抑制药，用于治疗成年T细胞白血病和毛细胞白血病。 コホリン静注用7.5mg 药物分类名称 抗肿瘤药 首次上市：1996年5月 商標名 Coforin 一般名 ペントスタチン（Pentostatin） 慣用名 2'-デオキシコホルマイシン、DCF 化学名 (R)-3-((2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol 分子式 C11H16N4O4 分子量 268.27 構造式 性状  Pentostatine是一种白色至微黄棕色粉末 药效药理 1. 抗肿瘤作用 在体内，尚未观察到对小鼠实验性肿瘤如P388，L1210等的影响，但已经报道了对大鼠实验性肿瘤的影响。 2. 作用机序 抑制素有效抑制腺苷脱氨酶。 当向活体施用喷司他丁时，具有抗肿瘤作用的腺苷衍生物如脱氧腺苷出现作为腺苷脱氨酶的抑制的结果，并且这些衍生物被认为具有抗肿瘤作用。 适应病症 （1）成人T细胞白血病淋巴瘤 （2）毛细胞白血病 用法与用量 在成人T细胞白血病淋巴瘤的情况下 通常，作为喷司他丁的4至5mg/m 2（体表面积）以一周的间隔静脉内施用4次。 让这个方法是一个过程，重复2到3的酷。 在毛细胞白血病的情况下 通常，每1至2周静脉内施用一次，每5至5mg/m 2。 在任一种情况下，对于患有肾损伤的患者测量肌酐清除率，并且在59至40mL/min的情况下将其调节至2至4mg/m 2，在39至25mL/min的情况下调节为1至3mg/m 2并以低剂量开始，并分别确认安全性。 注射液制备方法 注入连接到1瓶该产品上的7.5mL溶液并溶解。 包装规格 7.5mg *1小瓶（与7.5mL裂解溶液连接） 制造销售 日本化薬 完整说明书附件：http://www.info.pmda.go.jp/go/pack/4291404D1038_1_07/ Coforin（Pentostatin） A package insert Name of drug classification Antineoplastic agent common name Pentostatin Idiom 2'-deoxycoformycin, DCF Chemical name (R) -3 (2-deoxy-β-D-erythro-pento-furanosyl) -3,6,7,8-tetrahydroimidazo [4,5-d] [1,3] diazepin-8-ol Molecular formula C11 H 16 N 4 O 4 Molecular weight 268.27 Property Pentostatine is a white to pale yellowish white crystal or crystalline powder with no odor. It is easily soluble in water, hardly soluble in methanol or ethanol, and hardly soluble in ether. Melting point About 198 ° C (decomposition) Active ingredient Pentostatin 7.5 mg Additive Mannitol 37.5 mg Incidentally, the attached lysis solution contains 67.5 mg of sodium chloride in 1 vial 7.5 mL. Contraindication Patients with a history of severe hypersensitivity to this drug Patients with renal failure (patients with creatinine clearance <25 mL/min) [Renal failure may worsen] Patients with varicella or herpes zoster [There is a risk that varicella or herpes zoster may exacerbate due to immunosuppressive action] Patients receiving Vidarabine Injection (trade name: Arasena-A) [See "Interaction" section] Patients receiving cyclophosphamide or ifosfamide [See "Warning", "Interaction" section] Patients receiving fludarabine phosphate ester formulation [See "Warning", "Interaction" section] Pregnant women or lactating women who may be pregnant [See "Administration to pregnant women, maternity women, lactating women, etc."] Indication or effect Remission of subjective and objective symptoms of the following diseases Adult T cell leukemia lymphoma Hairy cell leukemia In the case of adult T cell leukemia lymphoma Usually, intravenously administer 4 to 5mg/m 2 (body surface area) as pentostatin four times at weekly intervals. Let this method be 1 cool and repeat 2 to 3 cool. In case of hairy cell leukemia Normally, 4 to 5mg/m 2 as pentostatin is intravenously administered once every 1 to 2 weeks. In any case, when there is renal disorder, creatinine clearance is measured, and when it is 59 to 40 mL/min, it is changed to 2 to 4mg/m 2, and in the case of 39 to 25 mL/min 1 to 3 mg/m 2 , And carefully administer them starting with a low dose and confirming the safety, respectively. Method for preparing injection solution Inject 7.5 mL of the solution attached to 1 vial of this product and dissolve. Careful Administration Patients with hepatic disorders [Liver disorder may worsen] Patients with renal impairment (patients with creatinine clearance 59-25 mL / min) [Renal disorder may worsen] Patients with cardiac dysfunction [There is a risk of cardiac function abnormality worsening] Patients with infectious disease combined [The immunosuppressive effect may cause the disease to worsen] Patients during allopurinol administration [See "Interaction" section] Senior citizens See "Administration to elderly people" section] Serious side effects Serious renal disorder Patients with kidney disorder have reported death due to hemolytic uremic syndrome (HUS: Hemolytic Uremic Syndrome) or renal failure, so frequent clinical examinations should be conducted to observe the patient's condition sufficiently. If abnormality is found, appropriate measures such as weight loss and withdrawal should be taken. Myelosuppression (Frequency unknown) Pancytopenia, leukopenia (granulocytopenia, neutropenia, lymphocytopenia), thrombocytopenia, anemia may appear or exacerbate, so observe thoroughly, frequently conducting blood tests, etc., and observe abnormalities If it is recognized, appropriate measures such as prolongation of dosing interval, reduction in weight and withdrawal should be taken. Medicinal pharmacology Antitumor effect In vivo, effects on mouse experimental tumors such as P388, L1210 and the like have not been observed, but effects on rat experimental tumors have been reported. Mechanism of action Pentostatin potently inhibits adenosine deaminase. When pentostatin is administered to a living body, adenosine derivatives having an antitumor effect such as deoxyadenosine appear as a result of inhibition of adenosine deaminase, and these derivatives are presumed to exert antitumor effect. Nipent治疗毛细胞性白血病可获得长期完全缓解 SuperGen公司宣称：一项长期随访研究的结果显示，SuperGen 公司生产的抗癌化合物pentostatin (Nipent) 可使毛细胞性白血病患者获得长期完全缓解。该项研究的结果发表在著名的血液学出版物《血液》杂志11月刊上。 Nipent 目前已由SuperGen 公司推向市场用于毛细胞性白血病的治疗。 由Johns Hopkins大学 Dr. Ian Flynn领导的该项研究共收集了从1986年12月至1989年9月间被诊断为毛细胞性白血病的241例患者。其中154例以Nipent作为初始治疗，87例以α-干扰素作为初始治疗无效后改为Nipent治疗。中位随访时间为9.3年，这项随访研究的目的是评价长期生存、无复发生存和并发恶性肿瘤的发生率。 应用Nipent作为初始治疗的病人，83％在11～14年后仍然存活，在201例可评价的病人中5年生存率达90％，10年生存率为81％。年龄小于55岁的患者10年生存率为93％，而年龄大于55岁者10年生存率为68％。参与研究的241例患者中有40例已经死亡，其中只有2例死亡与毛细胞性白血病有关。 SuperGen公司的主席Joseph Rubinfeld博士说：“来自这项长期随访研究的资料证实了我们的想法，即Nipent 是有效治疗毛细胞性白血病的一线药物。随着疾病自然史的延长，Nipent已经给毛细胞性白血病的治疗带来深刻影响。我们想将Nipent作为rubitecan和decitabine之外的第三个治疗各种血液肿瘤的技术平台。” 在今年早些时候由美国血液和骨髓移植学会举办的一次会议上，有资料显示了Nipent 治疗移植物抗宿主病（GVHD）的疗效。参与研究的9例病人有7例发生IV度GVHD，2例发生III度GVHD，以大剂量类固醇激素作为预防GVHD的最初治疗均无效。在应用Nipent 以前，许多病人应用环磷酰胺、FK506、ATG、MMF、Daclitumab和 Infliximab进行抢救均无效。而Nipent可很好地被病人耐受，并且，Nipent对其中4例病人完全有效，2例病人部分有效，总有效率为66％。