Brousil Julie A, Roberts Russel J, Schlein Amanda L
Department of Pharmacy Practice, St. Louis College of Pharmacy, St. Louis, MO 63110-1088, USA.
Ann Pharmacother. 2006 Oct;40(10):1814-21. doi: 10.1345/aph.1H037. Epub 2006 Sep 19.
To review the pharmacology, pharmacokinetics, efficacy, and safety of cladribine, a purine analog undergoing Phase III trials for approval of its use in the treatment of multiple sclerosis (MS).
A MEDLINE search (1966-September 2006) was conducted using the key words cladribine and multiple sclerosis. No limits were placed on the search.
Studies and review articles related to cladribine and MS were reviewed. The trials examining the role of cladribine in MS were analyzed.
Cladribine is a purine analog that demonstrates lymphocytotoxic activity. Recent data suggest that cladribine may have a role in the treatment of relapsing-remitting and the progressive forms of MS. In these studies, cladribine has shown mixed results in decreasing neurologic disability, as measured by various rating scales, but has consistently shown positive results in reducing the number of enhancing lesions, which reflects a measure of disease activity. To date, there is one ongoing study examining the role of oral cladribine in the treatment of relapsing-remitting MS. The incidence of adverse effects with cladribine has been significantly greater than with placebo, with the most common being myelosuppression.
While data do not support its use as a first-line MS treatment, cladribine may be a promising agent for refractory patients with secondary progressive MS. Further studies are warranted.
回顾克拉屈滨的药理学、药代动力学、疗效及安全性。克拉屈滨是一种嘌呤类似物，正处于III期试验阶段，以获批用于治疗多发性硬化症（MS）。
使用关键词“克拉屈滨”和“多发性硬化症”对MEDLINE数据库（1966年至2006年9月）进行检索。检索未设限制。
对与克拉屈滨和MS相关的研究及综述文章进行了回顾。分析了考察克拉屈滨在MS中作用的试验。
克拉屈滨是一种嘌呤类似物，具有淋巴细胞毒性活性。近期数据表明，克拉屈滨可能在复发缓解型和进展型MS的治疗中发挥作用。在这些研究中，通过各种评分量表衡量，克拉屈滨在降低神经功能残疾方面结果不一，但在减少强化病灶数量方面始终显示出阳性结果，强化病灶数量反映了疾病活动程度。迄今为止，有一项正在进行的研究考察口服克拉屈滨在复发缓解型MS治疗中的作用。克拉屈滨的不良反应发生率显著高于安慰剂，最常见的是骨髓抑制。
虽然现有数据不支持将其用作MS的一线治疗药物，但克拉屈滨对于继发进展型MS的难治性患者可能是一种有前景的药物。有必要进行进一步研究。
