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[克拉屈滨]

[Cladribine].

作者信息

Ogura Michinori

机构信息

Dept. of Hematology and Chemotherapy, Aichi Cancer Center Hospital, 1-1 Kanokoden, Chikusa-ku, Nagoya 464-8681, Japan.

出版信息

Gan To Kagaku Ryoho. 2003 Feb;30(2):309-17.

Abstract

Cladribine (2-chlorodeoxyadenosine: 2-CdA) is a chlorinated purine analogue that is resistant to degradation by adenosine deaminase. Phosphorylated derivatives of 2-CdA accumulate in lymphocytes with high deoxycytidine kinase activity, resulting in DNA strand breaks and cell death. Since the cytotoxic properties of 2-CdA are independent of cell division, 2-CdA is expected to be an effective agent in the treatment of indolent lymphoid malignancy with low-growth fraction. The agent was synthesized and has been investigated extensively by researchers at the Scripps Clinic and Research Foundation in the United States. The FDA approved cladribine for use against hairy cell leukemia, in 1993, and it was approved against hairy cell leukemia and indolent B-cell lymphoma in Japan in 2002 as Leustatin (Janssen Pharma Co. Ltd., Tokyo, Japan). The efficacy, toxicity and clinical usefulness of this agent against indolent lymphoid malignancies will be described according to the data from several clinical trials conducted in the United States, European countries and Japan.

摘要

克拉屈滨(2-氯脱氧腺苷:2-CdA)是一种氯化嘌呤类似物,对腺苷脱氨酶介导的降解具有抗性。2-CdA的磷酸化衍生物在具有高脱氧胞苷激酶活性的淋巴细胞中积累,导致DNA链断裂和细胞死亡。由于2-CdA的细胞毒性特性与细胞分裂无关,预计2-CdA将成为治疗低增殖分数惰性淋巴恶性肿瘤的有效药物。该药物已由美国斯克里普斯诊所及研究基金会的研究人员合成并进行了广泛研究。1993年,美国食品药品监督管理局(FDA)批准克拉屈滨用于治疗毛细胞白血病,2002年在日本,它作为Leustatin(日本东京杨森制药有限公司)被批准用于治疗毛细胞白血病和惰性B细胞淋巴瘤。本文将根据在美国、欧洲国家和日本进行的多项临床试验数据,描述该药物对惰性淋巴恶性肿瘤的疗效、毒性及临床应用价值。

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