Abstract
After the significant antileukemic effect of the pyrimidine nucleoside, 1-β-D- arabinofuranosylcytosine (ara-C), was recognized, efforts were made to identify other clinically active arabinosyl nucleosides. The purine nucleoside analogue, 9-β-D-arabinofurano-syladenine (ara-A), was found to be of little therapeutic value due to its rapid inactivation by adenosine deaminase (ADA) [1]. This metabolic obstacle is overcome, however, by the 2-fluoro derivative of ara-A, 9-β-D-arabinofuranosyl-2-fluoroadenine (F-ara-A), which is a relatively poor substrate for ADA [2] (figure 6-1). Because of the aqueous insolubility of the parent compound, F-ara-A, the more soluble 5′- monophosphate formulation, 9-β-D-arabinosylfuranosyl-2-fluoroadenine-5′- monophosphate (fludarabine phosphate, Fludara™ I.V.) has been used in clinical studies.
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Robertson, L.E., Keating, M.J. (1993). Fludarabine phosphate in the treatment of chronic lymphocytic leukemia: Biology, clinical impact, and future directions. In: Freireich, E.J., Kantarjian, H. (eds) Leukemia: Advances in Research and Treatment. Cancer Treatment and Research, vol 64. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-3086-2_6
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DOI: https://doi.org/10.1007/978-1-4615-3086-2_6
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