Cytochrome P450 binding studies of novel tacrine derivatives: Predicting the risk of hepatotoxicity.


The 1,2,3,4-tetrahydroacridine derivative tacrine was the first drug approved to treat Alzheimer's disease (AD). It is known to act as a potent cholinesterase inhibitor. However, tacrine was removed from the market due to its hepatotoxicity concerns as it undergoes metabolism to toxic quinonemethide species through the cytochrome P450 enzyme CYP1A2. Despite… (More)
DOI: 10.1016/j.bmcl.2017.04.006

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