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.
This is a preview of subscription content, access via your institution
Access options
Subscribe to this journal
Receive 24 print issues and online access
$259.00 per year
only $10.79 per issue
Buy this article
- Purchase on Springer Link
- Instant access to full article PDF
Prices may be subject to local taxes which are calculated during checkout
Similar content being viewed by others
Rights and permissions
About this article
Cite this article
Josephy, P., Palcic, B. & Skarsgard, L. In vitro metabolism of misonidazole. Br J Cancer 43, 443–450 (1981). https://doi.org/10.1038/bjc.1981.65
Issue Date:
DOI: https://doi.org/10.1038/bjc.1981.65
This article is cited by
-
Epigenetic modulation and apoptotic induction by a novel imidazo-benzamide derivative in human lung adenocarcinoma cells
DARU Journal of Pharmaceutical Sciences (2021)
-
Development of drugs based on imidazole and benzimidazole bioactive heterocycles: recent advances and future directions
Medicinal Chemistry Research (2016)
-
Distribution and tumor penetration properties of a radiosensitizer 2-[14C] misonidazole (Ro 07-0582), in mice and rats as studied by whole-body autoradiography
Cancer Chemotherapy and Pharmacology (1986)
