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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 55 mg/mL|
Antitumor activity of fludarabine against human multiple myeloma in vitro and in vivo.
Meng H, et al. Eur J Haematol. 2007 Dec;79(6):486-93. PMID: 17976186.
Fludarabine prevents smooth muscle proliferation in vitro and neointimal hyperplasia in vivo through specific inhibition of STAT-1 activation.
Torella D, et al. Am J Physiol Heart Circ Physiol. 2007 Jun;292(6):H2935-43. PMID: 17293493.
Fludarabine plus cyclophosphamide versus fludarabine alone in first-line therapy of younger patients with chronic lymphocytic leukemia.
Eichhorst BF, et al. Blood. 2006 Feb 1;107(3):885-91. PMID: 16219797.
Impact of frontline fludarabine and cyclophosphamide combined treatment on peripheral blood stem cell mobilization in B-cell chronic lymphocytic leukemia.
Tournilhac O, et al. Blood. 2004 Jan 1;103(1):363-5. PMID: 12969985.
In vitro evaluation of fludarabine in combination with cyclophosphamide and/or mitoxantrone in B-cell chronic lymphocytic leukemia.
Bellosillo B, et al. Blood. 1999 Oct 15;94(8):2836-43. PMID: 10515887.
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