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Monsarrat B, Maftouh M, Meunier G, et al. Oxidative biotransformation of the antitumour agent elliptinium acetate: Structural characterization of its human and rat urinary metabolites. J Pharm Biomed Anal. 1987;5(4):341-51doi: 10.1016/0731-7085(87)80040-7.
Monsarrat, B., Maftouh, M., Meunier, G., Bernadou, J., Armand, J. P., Paoletti, C., & Meunier, B. (1987). Oxidative biotransformation of the antitumour agent elliptinium acetate: Structural characterization of its human and rat urinary metabolites. Journal of pharmaceutical and biomedical analysis, 5(4), 341-51. https://doi.org/10.1016/0731-7085(87)80040-7
Monsarrat, B, et al. "Oxidative biotransformation of the antitumour agent elliptinium acetate: Structural characterization of its human and rat urinary metabolites." Journal of pharmaceutical and biomedical analysis vol. 5,4 (1987): 341-51. doi: https://doi.org/10.1016/0731-7085(87)80040-7
Monsarrat B, Maftouh M, Meunier G, Bernadou J, Armand JP, Paoletti C, Meunier B. Oxidative biotransformation of the antitumour agent elliptinium acetate: Structural characterization of its human and rat urinary metabolites. J Pharm Biomed Anal. 1987;5(4):341-51. doi: 10.1016/0731-7085(87)80040-7. PMID: 16867503.
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J Pharm Biomed Anal. 1987;5(4):341-51. doi: 10.1016/0731-7085(87)80040-7.

Oxidative biotransformation of the antitumour agent elliptinium acetate: Structural characterization of its human and rat urinary metabolites.

Journal of pharmaceutical and biomedical analysis

B Monsarrat, M Maftouh, G Meunier, J Bernadou, J P Armand, C Paoletti, B Meunier

Affiliations

  1. Laboratoire de Pharmacologie et Toxicologie Fondamentales du CNRS, 205 route de Narbonne, 31400 Toulouse, France.

PMID: 16867503 DOI: 10.1016/0731-7085(87)80040-7

Abstract

The electrophilic properties of the antitumour drug N(2)-methyl-9-hydroxyellipticinium acetate (Celiptium) are revealed by the detection of thiol-conjugate metabolites in man and rat urine. Besides the unchanged drug and its glucuronide, the cysteinyl- (in man) and the N-acetylcysteinyl- (in man and rat) conjugates have been unambiguously characterized using NMR, UV and mass spectral data. The urinary excretion profile exhibits total excreted products of 21% (in man) and 9% (in rat) with respect to the administered dose. The unchanged drug is found to be the major excreted compound from urine in both species (17% in man, 6.3% in rat); whereas the glucuronide (2.6% in man, 1.5% in rat), cysteinyl- (1.3% in man) and N-acetylcysteinyl- (0.2% in man, 1.2% in rat) conjugates represent the minor excreted compounds. The presence of the latter thio-conjugates provides an indirect proof of the in vivo generation of an oxidized intermediate form of the administered drug.

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