Covalent binding drug-related material

Table 1 Overall metabolic turnover and levels of covalent binding of drug-related material following incubation of compounds 4, 5, or 6 (10 pM) with rat and human liver microsomal preparations in the presence of NADPH at 37°C for 1 h...

The final issue arises from the fact that the extent of covalent binding observed in vivo in most cases likely will depend upon the magnitude of the systemic and liver exposure to drug-related material which, in turn, is dependent upon the physico-chemical properties, formulation, and pharmacokinetic and tissue distribution properties of the drug candidate. Although there is no simple way to precisely... 

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