This Article Full Text (PDF) Alert me when this article is cited Alert me if a correction is posted Services Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Citing Articles Citing Articles via Google Scholar Google Scholar Articles by LePage, G. A. Articles by Gottlieb, J. A. Search for Related Content PubMed PubMed Citation Articles by LePage, G. A. Articles by Gottlieb, J. A.

5'-Nucleotides as Potential Formulations for Administering Nucleoside Analogs in Man¹

The The University of Texas M. D. Anderson Hospital and Tumor Institute at Houston, Houston, Texas 77025

The kidneys of mice and other small mammals contain relatively high phosphomonoesterase levels. When 5'-nucleotides of 9-ß-D-arabinofuranosyladenine and 9-(ß-D-arabinofuranosyl)-6-mercaptopurine were administered to mice, they were rapidly dephosphorylated and excreted in the same form and at the same rate as if the nucleosides were given. However, human kidney samples had much lower phosphomonoesterase levels, and when 5'-nucleotides of the 2 nucleoside analogs were administered to patients they were relatively slowly converted to nucleosides and provided sustained blood plasma levels of the nucleosides. This appears to have potential advantages both for providing sustained dosage and for a better dosage formulation, the latter because of the greater solubility of the nucleotides.

¹ Aided by Grant T544 from the American Cancer Society.

² Present address: McEachern Laboratory, University of Alberta, Edmonton, Alberta, Canada.

Received 6/14/72. Accepted 8/ 2/72.