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Identification and Mitigation of Reactive Metabolites of 2‑Aminoimidazole-Containing Microsomal Prostaglandin E Synthase‑1 Inhibitors Terminated Due to Clinical Drug-Induced Liver Injury

Version 2 2018-02-22, 21:03
Version 1 2018-02-15, 18:03
Posted on 2018-02-22 - 21:03
Two 2-aminoimidazole-based inhibitors, LY3031207 (1) and LY3023703 (2), of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme were found to cause drug-induced liver injury (DILI) in humans. We studied imidazole ring substitutions to successfully mitigate reactive metabolite (RM) formation. These studies support the conclusion that RM formation may play a role in the observations of DILI and the consideration of 2-aminoimidazoles as structure alerts, due to the high likelihood of bioactivation to generate RMs.

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