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A Comprehensive Listing of Bioactivation Pathways of Organic Functional Groups.

Kalgutkar et al.  Current Drug Metabolism (2005), 6, 161-225.

Detailed studies of the metabolic fates of a range of drugs are surveyed and described. The focus is on the role that bioactivated compounds can have in causing toxicity and adverse drug reactions, particularly the idiosyncratic type of adverse reaction that cause many problems in the clinic that could not easily be predicted in advance. As shown in the graph, these also depend on the dose of the drug. The mechanism (where it is known) by which each transformation occurs and the enzyme(s) that catalyses it is indicated. Some idea of the generality of each reaction type is given where it is known but this is the big challenge in a review of this type – the number of examples that have been studied is so small that their scope cannot be elucidated. A valuable read to provide a good background in the sort of thing to look out for but also as a reminder to expect to be surprised!

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