TABLE 1

Summary of proposed metabolites observed in radiochromatogram (red trace in Fig. 2) and percentage of metabolism of SAM-760 in human hepatocytes

Peak NumberRt (min)m/zPutative IdentificationTotal Radioactivity from Metabolites1-ABT Sensitive?
min%
115.2143Benzenesulfinic acid43No
2∼18N.D.Unknown6.3No
319.7549Glucuronide of peak 54.5Yes
4∼27N.D.Unknown1.9Yes
530.1373Hydroxyl on methyl benzimidazole1.3Yes
633.0373Hydroxyl on methyl benzimidazole1.5Yes
SAM-76035.1357SAM-760N/AN/A
736.7389Carboxylic acid12Yes
838.5549Glucuronide of peak 97.2Yes
939.1373Hydroxylamine of piperazine1.3Yes
1041.3369Unknown2.0Yes
1141.8389Carboxylic acid1.7Yes
1245.3437Sulfamic acid on piperazine4.5No
1346.6373N-acetyl cysteine4.8Yes
1448.8288Cleaved piperzine5.8Yes
1550.0346Piperazine oxidation2.6Yes
  • N/A, not applicable; ND, not determined.