TABLE 2

Human metabolites detected in incubations with micropatterned human hepatocyte coculture compared with other in vitro human liver systems

There was 100% concordance in metabolite formation between the two separate micropatterned coculture studies. Data for hepatocytes, S9, and microsomes are taken from Dalvie et al., 2009.

Compound	In Vivo Human Metabolites	Metabolites Detected
		Hepatocytes	S9	Microsomes	Micropatterned Coculture Incubated
		Hepatocytes	S9	Microsomes	48 h	7 day
Gemcabene	Gemcabene glucuronide	No	No	No	Yes	Yes
Avasimibe	Dehydrogenated avasimibe	No	No	No	Yes	Yes
	Hydroxyavasimibe	No	No	No	No	No
Pagoclone	Hydroxypagoclone	Yes	Yes	No	Yes	Yes
Axitinib	Hydroxyaxitinib	Yes	Yes	Yes	Yes	Yes
	Axitinib sulfoxide	Yes	Yes	Yes	Yes	Yes
	Axitinib glucuronide	Yes	No	No	Yes	Yes
Capravirine	Hydroxycapravirine sulfoxide	Yes	Yes	Yes	Yes	Yes
	Hydroxycapraivirinesulfone N-oxide	Yes	Yes	No	Yes	Yes
CJ-13610	CJ-13610 sulfoxide	Yes	Yes	Yes	Yes	Yes
	CJ-13610 sulfone	Yes	Yes	Yes	Yes	Yes
Traxoprodil	Traxoprodil methoxy sulfate	Yes	No	No	Yes	Yes
	Traxoprodil methoxy glucuronide	Yes	No	No	Yes	Yes
CP-122721	Desmethyl CP-122721 glucuronide	Yes	Yes	Yes	Yes	Yes
	N-Dealkylated CP-122721 glucuronide	No	No	No	No	No
	Desmethylhydroxy CP-122721 glucuronide	No	No	No	No	No
	5-Trifluoromethoxysalicylic acid	No	No	No	No	No
Tofimulast	Dihydroxytofimulast	No	Yes	Yes	Yes	Yes
	Ring-opened tofimulast	Yes	Yes	No	Yes	Yes
	Desthiophene tofimulast	No	No	No	Yes	Yes
Lasofoxifene	Lasofoxifene glucuronide	Yes	Yes	Yes	Yes	Yes
Capromorelin	Carboxylic acid of capromorelin	No	No	No	No	No
	O-Debenzyl hydroxycapromorelin	No	No	Yes	Yes	Yes
	Carboxylic acid of N-desmethyl-O-debenzylcapromorelin	No	No	No	No	No
	N-Desmethyl-O-debenzyl hydroxycapromorelin	No	No	No	Yes	Yes
Torcetrapib	Bistrifluoromethyl benzoic acid	No	No	No	No	No
	7-Trifluoromethylquinaldic acid	No	Yes	Yes	Yes	Yes
CP-533536	Hydroxy CP-533536	Yes	Yes	Yes	Yes	Yes
	CP-533536 sulfate	No	No	No	Yes	Yes
CP-547632	N-Dealkyl CP-547632	No	No	No	No	No
Zoniporide	Hydroxyzoniporide	Yes	Yes	Yes	Yes	Yes
	Zoniporide carboxylic acid	Yes	No	No	No	Yes
Celecoxib	Carboxylic acid of celecoxib	Yes	Yes	No	Yes	Yes
	Celecoxib glucuronide	Yes	No	No	Yes	Yes
CP-690550	Hydroxy CP-690550	No	No	Yes	No	Yes
	Dihydroxy CP-690550	Yes	Yes	Yes	Yes	Yes
	Dihydroxy CP-690550 glucuronide	No	No	No	No	No
Ziprasidone	Ziprasidone sulfoxide	Yes	Yes	Yes	Yes	Yes
	S-Methyldihydroziprasidone	Yes	Yes	No	Yes	Yes
	N-Dealkylziprasidone S-oxide	No	No	No	Yes	Yes
	N-Dealkylziprasidone sulfone	No	No	No	No	No
Sunepitron	Hydroxysunepitron	Yes	Yes	Yes	Yes	Yes
Trovafloxacin	Trovafloxacin glucuronide	Yes	Yes	Yes	No	Yes
Linezolid	Ring-opened linezolid	No	No	No	No	Yes
	Ring-opened linezolid	No	No	No	No	Yes
Sunitinib	N-Dealkyl sunitinib	Yes	Yes	Yes	Yes	Yes
Irinotecan	Ring-opened carboxylic acid	Yes	Yes	Yes	Yes	Yes
Delavirdine	N-Dealkyldelavirdine	Yes	Yes	Yes	Yes	Yes
	Depyridinyl delavirdine	No	No	No	No	No
Valdecoxib	Hydroxyvaldecoxib glucuronide	Yes	Yes	No	Yes	Yes
	Valdecoxib N-glucuronide	Yes	No	No	Yes	Yes
Eplerenone	6β-Hydroxyeplerenone	Yes	Yes	Yes	Yes	Yes
	6β,21-Dihydroxeplerenone	Yes	No	No	No	No
Maraviroc	Hydroxymethyl maraviroc	Yes	Yes	Yes	Yes	Yes
	N-Desalkyl maraviroc	No	No	No	No	No
	N-Desalkyl hydroxymethyl maraviroc	No	No	No	Yes	Yes