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Fludarabine

氟達拉濱
Mechanism of action:
Fludarabine 是一種氟化嘌呤核苷(fluorinated purine nucleoside)類似物。Fludarabine 進入細胞後,先轉化為氟達拉濱單磷酸(fludarabine monophosphate),再經細胞的激酶磷酸化為氟達拉濱三磷酸(fludarabine triphosphate),此為主要的活性抗癌形式。氟達拉濱三磷酸能抑制多個與 DNA 合成相關的關鍵酵素,包含 DNA 聚合酶-α、δ、ε、核糖核苷酸還原酶(ribonucleotide reductase)、DNA 引發酶(DNA primase)等,使細胞的 DNA 合成異常,最後導致細胞凋亡。
Reference(s):
1. Rai KR et al. (2000). Fludarabine compared with chlorambucil as primary therapy for chronic lymphocytic leukemia. N Engl J Med.
2. Gonzalez H et al. (1998). Severe autoimmune hemolytic anemia in eight patients treated with fludarabine. Hematol Cell Ther.
3. Tournilhac O et al. (2004). Impact of frontline fludarabine and cyclophosphamide combined treatment on peripheral blood stem cell mobilization in B-cell chronic lymphocytic leukemia. Blood.
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