Fludarabine

Fludarabine (Fludara) is a purine analog that inhibits DNA synthesis. Fludarabine is used in the treatment of hematological malignancies (cancers of blood cells such as leukemias and lymphomas). Fludarabine inhibits DNA synthesis by interfering with ribonucleotide reductase and DNA polymerase. Fludarabine markedly inhibited VSMC proliferation in cell culture. Furthermore, fludarabine reduced neointimal formation after balloon angioplasty in a dose-dependent manner, and fludarabine-eluting stents reduced neointimal hyperplasia by approximately 50%. Fludarabine induces apoptosis of cancer cells and RNA transcription inhibitor. Fludarabine also induces significant reduction of STAT-1 phosphorylation, whereas it does not change JAK2 activation. Fludarabine exhibits antiproliferative activity (IC50 = 1.54 μM in RPMI cells) and triggers apoptosis through increasing Bax and decreasing Bid, XIAP and survivin expression. Fludarabine displays anticancer activity against hematological malignancies in vivo.