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Clofarabine

氯法拉濱

Mechanism of action:

Clofarabine 是一種嘌呤核苷（purine nucleoside）類似物。Clofarabine 能在細胞內被轉化為活性代謝物 clofarabine triphosphate，可被誤認為去氧腺苷三磷酸（dATP）而摻入 DNA 中。雖然 clofarabine 有 3'-OH 基團，但由於其糖構型是 arabinose，被摻入後常使後續的 DNA 延長效率大幅下降或中止（與其 arabinose 構型及分子取代基造成的立體/酵素相容性不佳有關），能進一步抑制細胞分裂。Clofarabine 也會抑制核糖核苷酸還原酶（ribonucleotide reductase）的活性，阻止 dNTP 的生成。

​Reference(s):

1. Pession A et al. (2010). Use of clofarabine for acute childhood leukemia. Biologics. 


2. Harned TM et al. (2008). Treating refractory leukemias in childhood, role of clofarabine. Ther Clin Risk Manag. 


3. Lech-Maranda E et al. (2009). Clofarabine as a novel nucleoside analogue approved to treat patients with haematological malignancies: mechanism of action and clinical activity. Mini Rev Med Chem.

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