IMR Press / FBE / Volume 4 / Issue 6 / DOI: 10.2741/e525

Frontiers in Bioscience-Elite (FBE) is published by IMR Press from Volume 13 Issue 2 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on imrpress.com as a courtesy and upon agreement with Frontiers in Bioscience.

Open Access Review

Arylamine drugs: genotoxic-carcinogenic activity of NO-derivatives

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1 Department of Internal Medicine, Division of Clinical Pharmacology and Toxicology, University of Genoa, Viale Benedetto XV, 2, I-16132 Genoa, Italy

Academic Editor: King-Thom Chung

Front. Biosci. (Elite Ed) 2012, 4(6), 2071–2084; https://doi.org/10.2741/e525
Published: 1 January 2012
(This article belongs to the Special Issue Arylamine induced carcinogenesis)
Abstract

This review provides information on arylamine drugs which have been tested for the formation of Nnitroso compounds (NOC) by reacting with nitrite, and on the genotoxic-carcinogenic effects of their nitrosation products. In an extensive search we have found that 109 arylamine drugs were examined for their ability to react with nitrite, and 105 of them (96.3%) were found to form NOC or in some cases other reactive species. Moreover, 78 arylamine drugs were examined in short-term genotoxicity tests and/or in long-term carcinogenicity assays, either in combination with nitrite or using their nitrosation product; 67 of them (85.9%) have been found to give at least one positive response. Only a small fraction, the 19.1% of theoretically nitrosatable arylamine drugs, has been examined for the possible formation of genotoxiccarcinogenic NOC, guidelines for genotoxicity testing of pharmaceuticals do not indicate the need of appropriate tests, and patients are not informed that the drug-nitrite interaction and the consequent risk can be reduced to a large extent by consuming the nitrosatable drug with ascorbic acid.

Keywords
Arylamine drugs
NO-derivatives
Genotoxiccarcinogenic activity
Review
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