Category Archives: Toxicology

Drug discovery approaches to minimise drug induced liver injury in man

The recent literature has seen a flurry of papers describing the issue of, and potential approaches to minimising the incidence of, drug-induced liver injury (DILI) in the clinic.   It is well recognised that attrition throughout the development pipeline is often … Continue reading

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Reducing bioactivation potential by chemical design

Continuing the theme of an earlier post, an excellent article in Current Topics in Medicinal Chemistry looks at the issue of adverse drug events associated with the formation of reactive intermediates.  The authors (from Novartis) give some background to drug-related … Continue reading

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Review: Chemical carcinogenicity and mutagenicity

A new review, titled ‘Mechanisms of chemical carcinogenicity and mutagenicity: a review with implications for predictive toxicology’ , collates the experimentally derived mechanistic knowledge relating to this type of chemically induced toxicity.  Whilst a lot of the material is well … Continue reading

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Structural Alert: Benzimidazoles

An informative letter, just published by a team from Novartis, highlights the risk of suitably substituted benzimidazoles acting as latent precursors to reactive ortho-iminoquinone species.  The example they report (see structure on left below) was Ames positive and exhibited time-dependent inhibition … Continue reading

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