Table 3.
Potential metabolites of gefitinib, losartan, and SSRIs: citalopram, fluoxetine, fluvoxamine, paroxetine, sertraline, and venlafaxine from hepatocytes and CYP1A2, 2C9, 2C19, 2D6, and 3A4 screening. Observed potential metabolite is recorded as “+“. Potential metabolites were previously described for gefitinib (McKillop et al., 2004, 2005), losartan (Sica et al., 2005), citalopram (Sangkuhl et al., 2011), fluoxetine (Deodhar et al., 2021), fluvoxamine (van Harten, 1995), sertraline (Obach et al., 2005; DeVane et al., 2002), and venlafaxine (Sangkuhl et al., 2014).
Parent Drugs | Metabolites Information | Potential Metabolite | Hepatocytes | CYP 1A2 | CYP 2C9 | CYP 2C19 | CYP 2D6 | CYP 3A4 |
---|---|---|---|---|---|---|---|---|
Gefitinib (m/z-447) | Demethylation | m/z-433 | + | + | + | + | ||
Dehydrogenation | m/z-445 | + | + | |||||
(+25 amu) | m/z-472 | + | + | + | + | + | ||
Losartan (m/z-423) | N-Oxidation | m/z-439 | + | + | + | |||
Citalopram (m/z-325) | Demethylation | m/z-311 | + | + | + | + | + | |
N- Methylation | m/z-338 | + | + | + | ||||
N-Oxidation | m/z-341 | + | + | + | + | + | ||
(+27 amu) | m/z-352 | + | + | + | + | + | ||
Fluoxetine (m/z-310) | Demethylation | m/z-296 | + | + | ||||
(+27 amu) | m/z-337 | + | + | + | + | |||
Fluvoxamine (m/z-319) | Demethylation | m/z-305 | + | + | ||||
(+27 amu) | m/z-346 | + | + | |||||
Sertraline (m/z-306) | Demethylation | m/z-292 | + | + | + | + | + | + |
(+27 amu) | m/z-333 | + | + | + | + | + | + | |
Venlafaxine (m/z-278) | Demethylation | m/z-264 | + | + | + | |||
(+27 amu) | m/z-305 | + | + |