The P450 type cytochromes are responsible for the metabolism of a wide variety of
xenobiotics and endogenous compounds. Although P450-catalyzed reactions are generally …

It is generally accepted that bioactivation of relatively inert functional groups (toxicophores)
to reactive metabolites is an obligatory step in the pathogenesis of certain idiosyncratic …

In vitro metabolism/bioactivation of structurally related central nervous system agents
nefazodone (hepatotoxin) and aripiprazole (nonhepatotoxin) were undertaken in human …

A need still exists for a liquid chromatography/tandem mass spectrometry (LC/MS/MS)
method that can detect broad classes of glutathione (GSH) conjugates and provide …

Drug induced toxicity remains one of the major reasons for failures of new pharmaceuticals,
and for the withdrawal of approved drugs from the market. Efforts are being made to reduce …

We describe a novel peptide-based in vitro method for the detection of reactive metabolites
that is amenable for use with microsomal or purified enzyme systems. Covalently bound …

It has become widely accepted that in vitro metabolism studies can play a useful roleduring
the nonclinical testing of novel chemical entities (NCEs)(1-7). Therefore, mostresearchers …

Today's pharmaceutical industry is under a tremendous amount of pressure to cutoperating
costs, reduce cycle times for drug discovery and development, and deliver safeand effective …

The drug discovery and development processes are time consuming and costly endeavors.
It has been reported that on average it takes 10 to 15 years and costs more than $800 …

抄録 A large number of electrophilic reactive metabolites, such as quinone derivatives,
Michael acceptors, nitrogen-containing electrophiles, and epoxides, are produced from drug …