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. 1981 Apr;43(4):443–450. doi: 10.1038/bjc.1981.65

In vitro metabolism of misonidazole.

P D Josephy, B Palcic, L D Skarsgard
PMCID: PMC2010618  PMID: 7236487

Abstract

Misonidazole (MISO) is a nitroimidazole drug currently undergoing clinical trials as a radiosensitizer of hypoxic tumour cells. The drug is also toxic to such cells, probably because of metabolic activation of the nitro group under hypoxia. The metabolic fate of 14C-labelled MISO is examined, using hypoxic mammalian (CHO) cells in vitro. Organic-soluble and acid-soluble metabolites are formed, and radioactivity is bound to macromolecules. The organic-soluble products are separated by TLC and HPLC. Evidence is presented to show that one of the metabolites is hydroxylamino-misonidazole. The significance of metabolic nitroreduction is discussed.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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