Table 2.

Kinetic parameters for MEGX activities of wild-type and 22 CYP3A4 allelic variants against lidocaine

Variants	Vmax (pmol/min/pmol P450)	Km (µM)	Intrinsic clearance (Vmax/Km)	Relative clearance (% of wild type)
CYP3A4*1	7,885.00±245.95	471.80±62.71	16.98±1.63	100.00
CYP3A4*2 (S222P)	4,015.00±30.44**	842.03±38.09**	4.73±0.19**	27.93**
CYP3A4*3 (M445T)	11,350.00±153.08**	639.57±24.81*	18.04±0.49	106.61
CYP3A4*4 (I118V)	8,442.00±824.33	542.17±169.20	14.80±3.21	85.95
CYP3A4*5 (P218R)	6,436.00±265.43**	1,103.67±124.03**	5.60±0.41**	32.99**
CYP3A4*9 (V170I)	8,304.00±272.52	713.40±51.53**	11.52±0.47**	67.93**
CYP3A4*10 (D174H)	10,730.00±523.55**	554.43±157.91	19.09±3.96	109.93
CYP3A4*11 (T363M)	27,020.00±2,343.67**	702.57±167.08	36.42±5.47**	213.61**
CYP3A4*14 (L15P)	10,120.00±317.96**	406.63±27.76	25.65±1.00**	151.58**
CYP3A4*15 (R162Q)	10,730.00±683.04**	491.07±41.54	20.87±0.47*	123.27*
CYP3A4*16 (T185S)	6,804.00±202.09**	812.23±56.71**	8.11±0.52**	47.91**
CYP3A4*17 (F189S)	ND	ND	ND	ND
CYP3A4*18 (L293P)	13,470.00±217.79**	493.97±32.27	27.20±1.55**	160.51**
CYP3A4*19 (P467S)	9,887.00±325.53**	466.17±99.43	22.40±4.01	130.35*
CYP3A4*23 (R162W)	10,560.00±195.53**	296.73±4.99**	35.04±0.77**	206.96**
CYP3A4*24 (Q200H)	304.60±10.90**	70.83±40.25**	4.93±2.15**	30.29**
CYP3A4*28 (L22V)	5,224.00±58.29**	290.60±25.19**	17.87±1.73	105.29
CYP3A4*29 (F113I)	7,771.00±344.40	310.00±42.34*	24.08±2.28*	141.84*
CYP3A4*30 (R130STOP)	ND	ND	ND	ND
CYP3A4*31 (H324Q)	7,949.00±99.96	237.30±20.46**	33.58±2.89**	197.87**
CYP3A4*32 (I335T)	8,743.67±482.94**	289.60±46.99**	30.74±5.18**	182.56**
CYP3A4*33 (A370S)	4,865.00±130.48**	328.23±24.17*	14.43±0.70	85.16
CYP3A4*34 (I427V)	12,225.67±1,244.09**	532.50±343.48**	28.15±12.35**	154.49**

Note: Significantly different from wild-type CYP3A4,

^*P<0.05,

^**P<0.01.

Abbreviations: MEGX, monoethylglycinexylidide; ND, not determined.