Introduction: A number of withdrawn drugs are known to undergo bioactivation by a range of
drug metabolizing enzymes to chemically reactive metabolites that bind covalently to protein …

Drug metabolism can result in the formation of highly reactive metabolites that are known to
play a role in toxicity resulting in a significant proportion of attrition during drug development …

Gefitinib (GEF), an inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, is
widely used for the treatment of cancers, particularly non-small cell lung cancer. However, its …

A novel class of benzoheterocyclic analogues of amodiaquine designed to avoid toxic
reactive metabolite formation was synthesized and evaluated for antiplasmodial activity …

Biotransformation is one of the key elements of chemically induced toxicity. Although
organisms have an intrinsic tendency to diminish the harm posed by chemical exposure with …

Idiosyncratic drug toxicity has led to the market withdrawal of many drugs in the past. Since
animal experiments are not predictive of such toxicity, the pharmaceutical industry continues …

Over the past decades, it has become abundantly clear that enzymes evolved to detoxify
and eliminate foreign chemicals from the body, occasionally generate highly reactive …

Introduction Glutathione (GSH) trapping assays are widely used to predict the post-
marketing risk for idiosyncratic drug reactions (IDRs) in the pharmaceutical industry …

Qualitative trapping profile of reactive metabolites arising from six structurally different
compounds was tested with three different d-peptide isomers (Peptide 1, gly–tyr–pro–cys …

Drug metabolism is one of the most important events a drug faces after administration.
Traditionally, drug metabolism has only been considered as a major clearance and …