TABLE 1

Kinetic parameters of CYP3A TDI in human liver microsomes and comparison with literature values

Drug	Novartis		Literature		Reference
Drug	k_inact	K_I	k_inact	K_I	Reference
	min⁻¹	μM	min⁻¹	μM
Amprenavir	0.174	1.9	0.450	0.64	Zhao et al. (2005)
Azamulin	>0.1	<0.5	0.680	0.17	Perloff et al. (2009)
Azithromycin	nTDI	>50	0.016	623	Ito et al. (2003)
Clarithromycin	0.058	13.2	0.072	4.5	Mayhew et al. (2000)
			0.019	15.5	Watanabe et al. (2007)
			0.036	41.5	Ito et al. (2003)
			0.063	15.7	Xu et al. (2009)
Diltiazem	0.031	3.6	0.012	4.5	Obach et al. (2007)
			0.050	8.7	Perloff et al. (2009)
			0.012	0.48	Zhao et al. (2005)
			0.015	18.1	McConn et al. (2004)
			0.019	0.67	Xu et al. (2009)
Diltiazem-N-desmethyl	0.043	0.8	0.027	0.77	Mayhew et al. (2000)
Domperidone	0.018	4.7	0.037	12	Chang et al. (2010)
Erythromycin	0.041	26.5	0.025	13.5	Ito et al. (2003)
			0.067	812	Yamano et al. (2001)
			0.072	15.2	Zhao et al. (2005)
			0.022	12.1	Watanabe et al. (2007)
			0.036	10	Obach et al. (2007)
			0.045	10.9	McConn et al. (2004)
			0.017	1.7	Xu et al. (2009)
Fluoxetine	nTDI	>50	0.017	5.3	Mayhew et al. (2000)
Isoniazid	nTDI	>50	0.080	228	Wen et al. (2002)
Nicardipine	>0.1	<0.5	0.060	1.3	McConn et al. (2004)
Paroxetine	nTDI	>50	0.011	13	Obach et al. (2007)
Pioglitazone	0.013	13.0	0.011	10.4	Lim et al. (2005)
Raloxifene	0.163	4.3	0.360	18.7	Zhao et al. (2005)
Ritonavir	>0.1	<0.5	0.450	0.38	Obach et al. (2007)
Rosiglitazone	0.011	4.4	0.020	11.9	Lim et al. (2005)
ThioTEPA	nTDI	>50	0.035	300	Obach et al. (2007)
Ticlopidine	0.008	3.5	0.039	77	Obach et al. (2007)
Troglitazone	0.087	10.0	0.034	5	Lim et al. (2005)
Troleandomycin	0.141	0.6	0.065	0.19	Xu et al. (2009)
			0.032	2.4	Zhao et al. (2005)
Verapamil	0.070	2.4	0.028	2.6	Watanabe et al. (2007)
			0.043	1.8	Obach et al. (2007)
			0.023	2	Perloff et al. (2009)
			0.053	3.5	Xu et al. (2009)

nTDI, no TDI effect at highest concentration investigated.