How to Choose In Vitro Systems to Predict In Vivo Drug Clearance: A System Pharmacology Perspective

Table 2

Predicted value and observed in vivo value of probe drugs.

Drug	Expression systems	The predicted value (L/h)	The observed in vivo value (L/h)	Scaling factor
Caffeine	Baculovirus	1.21	5.88	2.28
(R)-Lansoprazole (dexlansoprazole)	Baculovirus	81.74	18.48	−2.12
(R)-Omeprazole	Baculovirus	31.81	35.28	0.15
(R)-Omeprazole	Lymphoblastoid	15.56	35.28	1.18
(R)-Warfarin	Baculovirus	0.66	0.231	−1.51
(R)-Warfarin	E.coli	0.0041	0.231	5.82
(R)-Warfarin	Lymphoblastoid	0.018	0.1512	3.07
7-Epi-10-deacetyl-paclitaxel	Baculovirus	1.77	26.88	3.93
Alfentanil	Baculovirus	56.32	16.38	−1.79
Astemizole	Yeast	40.24	82.6	1.04
Atomoxetine	Baculovirus	1.65	20.99875	3.67
Bupropion	Baculovirus	7.27	5.415	−0.43
Celecoxib	Lymphoblastoid	41.26	21.05	−0.97
Celecoxib	Yeast	5.66	21.05	1.90
Cisapride	Baculovirus	20.76	14.1975	−0.56
Clobazam	Baculovirus	23.02	2.49	−3.18
Cyclosporine	Baculovirus	29.07	31.5	0.11
Dextromethorphan	Baculovirus	11.53	15.435	0.42
Dextromethorphan	E.coli	0.26	15.435	5.89
Dextromethorphan	Lymphoblastoid	11.87	15.435	0.38
Dextromethorphan	Yeast	21.66195	15.435	−0.49
Efavirenz	Baculovirus	0.19	5.483	4.85
Felodipine	Lymphoblastoid	0.83	46.2	5.80
Indinavir	Baculovirus	89.11	75.6	−0.23
Maraviroc	Baculovirus	33.78	44	0.38
Melatonin	Baculovirus	35.52	57.96	0.70
Metoprolol	Lymphoblastoid	44.05	54.6	0.31
Midazolam	Baculovirus	54.9	22.26	−1.29
Midazolam	E.coli	44.97	22.26	−1.03
Midazolam	Lymphoblastoid	46.51	22.26	−1.06
Perphenazine	Baculovirus	34.35	113.4	1.72
Phenytoin	Baculovirus	0.37	3.906	3.40
Phenytoin	Lymphoblastoid	1.07	3.906	1.87
Pimozide	Baculovirus	6.87	0.042471	−6.64
Quinidine	Lymphoblastoid	76.93	16.8	−2.18
Repaglinide	Baculovirus	27.29	32.76	0.26
Sildenafil	Baculovirus	5.17	38.22	2.89
Sirolimus	Baculovirus	19.47	2.73	−2.84
Tacrine	Yeast	16.96	235.2	3.79
Tacrolimus	Baculovirus	89.11	4.634	−4.32
Theophylline (1,3-DMX)	E. coli	6.6	3.612	−0.86
Theophylline (1,3-DMX)	Lymphoblastoid	8.04	3.612	−1.15
Tolterodine	baculovirus	2.22	10.5	2.24
Triazolam	Baculovirus	46.65	12.6	−1.89
Triazolam	Lymphoblastoid	4.65	12.6	1.44
Vardenafil	Baculovirus	27.75	54.6	0.98
Venlafaxine	Lymphoblastoid	13.91	40.95	1.56
Venlafaxine	Yeast	2.76	40.95	3.89