TABLE 1

Metabolites for the 27 compounds used in this analysis and their amount in human circulation and excreta

The amount in circulation or excreta are included only if values exceed 10%.

Compound NameIn Vivo Human MetabolitesPhase 1 or 2Primary or Secondary MetabolitePercentage in ExcretaPercentage of Circulating Radioactivity
GemcabeneGemcabene glucuronide2144
AvasimibeDehydrogenated avasimibe1116
Hydroxyavasimibe1110
PagocloneHydroxypagoclone1165
AxitinibHydroxyaxitinib1111
Axitinib sulfoxide1116
Axitinib glucuronide2150
CapravirineHydroxycapravirine sulfoxide1211
Hydroxycapraivirinesulfone N-oxide1210
CJ-13610CJ-13610 sulfoxide113617
CJ-13610 sulfone122110
TraxoprodilTraxoprodil methoxy sulfate224028
Traxoprodil methoxy glucuronide221018
CP-122721Desmethyl CP-122721 glucuronide222714
N-Dealkylated CP-122721 glucuronide2211
DesmethylhydroxyCP-122721 glucuronide2225
5-Trifluoromethoxysalicylic acid1256
TofimulastDihydroxytofimulast122314
Ring-opened tofimulast1233
Desthiophene tofimulast1213
LasofoxifeneLasofoxifene glucuronide2122
CapromorelinCarboxylic acid of capromorelin121114
O-Debenzyl hydroxycapromorelin1212
Carboxylic acid of N-desmethyl-O-debenzylcapromorelin1212
N-Desmethyl-O-debenzyl hydroxycapromorelin1215
TorcetrapibBistrifluoromethyl benzoic acid125050
7-Trifluoromethylquinaldic acid122963
CP-533536Hydroxy CP-5335361170
CP-533536 sulfate2111
CP-547632N-Dealkyl CP-5476321115
ZoniporideHydroxyzoniporide115264
Carboxylic acid of zoniporide1217
CelecoxibCarboxylic acid of celecoxib127320
Celecoxib glucuronide2215
CP-690550Hydroxy CP-690550112012
Dihydroxy CP-690550121212
Dihydroxy CP-690550 glucuronide221113
ZiprasidoneZiprasidone sulfoxide111869
S-Methyldihydroziprasidone121869
N-Dealkylziprasidone S-oxide121121
N-Dealkylziprasidone sulfone121121
SunepitronHydroxysunepitron111761
TrovafloxacinTrovafloxacin glucuronide211322
LinezolidRing-opened linezolid1245
Ring-opened linezolid1210
SunitinibN-Dealkyl sunitinib113221
IrinotecanRing-opened carboxylic acid1211
DelavirdineN-Dealkyldelavirdine114625
Depyridinyl delavirdine1138
ValdecoxibHydroxyvaldecoxib glucuronide2223
Valdecoxib N-glucuronide2120
Eplerenone6β-Hydroxyeplerenone113216
6β,21-Dihydroxeplerenone1221
MaravirocHydroxymethyl maraviroc1113
N-Desalkyl maraviroc1222
N-Desalkyl hydroxymethyl maraviroc1211