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Cladribine

克拉屈濱
Mechanism of action:
Cladribine 是一種嘌呤核苷(purine nucleoside)類似物,需經細胞內的去氧胞苷激酶(deoxycytidine kinase)磷酸化為 cladribine monophosphate,之後再由其他激酶陸續磷酸化成 cladribine triphosphate。在細胞進行 DNA 合成時,cladribine triphosphate 有機會被嵌入 DNA 中,造成 DNA 合成與修復受干擾、DNA 損傷與斷裂累積,促使細胞凋亡。因為淋巴細胞中的去氧胞苷激酶表達量特別高,所以會造成 T、B 淋巴球大量凋亡。
Reference(s):
1. Sigal DS et al. (2010). Beyond hairy cell: the activity of cladribine in other hematologic malignancies. Blood.
2. Pfeuffer S et al. (2022). Effectiveness and safety of cladribine in MS: Real-world experience from two tertiary centres. Mult Scler.
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