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 HighWire Citing Articles via Google Scholar Google Scholar Articles by Zimmerman, T. P. Articles by Elion, G. B. Search for Related Content PubMed PubMed Citation Articles by Zimmerman, T. P. Articles by Elion, G. B.

Identification of 6-Methylmercaptopurine Ribonucleoside 5'-Diphosphate and 5'-Triphosphate as Metabolites of 6-Mercaptopurine in Man

The Wellcome Research Laboratories, Research Triangle Park, North Carolina 27709

Acid-soluble extracts of bone marrow and blood samples from leukemia patients receiving 6-mercaptopurine were analyzed by anion-exchange high-pressure liquid chromatography. This has led to the identification of two previously unrecognized metabolites of 6-mercaptopurine, 6-methylmercaptopurine ribonucleoside 5'-diphosphate and the corresponding 5'-triphosphate. Intracellular concentrations of 6-methylmercaptopurine ribonucleoside 5'-triphosphate often exceeded those of either the corresponding 5'-mono- or 5'-diphosphate and were estimated to be as high as 145 µM. There is no evidence at present that these newly reported metabolites of 6-mercaptopurine are themselves highly cytotoxic, but they may perhaps contribute to the overall cytotoxicity of 6-mercaptopurine.

Received 8/13/73. Accepted 10/19/73.

This article has been cited by other articles:

				G. Zaza, M. Cheok, W. Yang, J. C. Panetta, C.-H. Pui, M. V. Relling, and W. E. Evans Gene expression and thioguanine nucleotide disposition in acute lymphoblastic leukemia after in vivo mercaptopurine treatment Blood, September 1, 2005; 106(5): 1778 - 1785. [Abstract] [Full Text] [PDF]

				T. Dervieux, Y. Chu, Y. Su, C.-H. Pui, W. E. Evans, and M. V. Relling HPLC Determination of Thiopurine Nucleosides and Nucleotides in Vivo in Lymphoblasts following Mercaptopurine Therapy Clin. Chem., January 1, 2002; 48(1): 61 - 68. [Abstract] [Full Text] [PDF]