TABLE 1

Raloxifene glucuronidation kinetics

Values represent the parameter estimate ± S.E obtained by fitting the Michaelis–Menten equation (eq. 1) to metabolite (R4G or R6G) formation velocity using Phoenix WinNonlin software (version 6.3). CL_int is calculated as the ratio of V_max to K_m.

Enzyme Source	R4G			R6G
Enzyme Source	K_m	V_max	CL_int	K_m	V_max	CL_int
	µM	pmol/min per mg	µl/min per mg	µM	pmol/min per mg	µl/min per mg
HIMs	0.81 ± 0.11	750 ± 22	930	0.84 ± 0.14	78 ± 2.9	93
HLMs	3.0 ± 0.73	850 ± 53	290	6.5 ± 0.73	310 ± 9.7	48
UGT1A1	4.3 ± 0.51	88 ± 2.7	20	3.6 ± 0.39	92 ± 2.4	26
UGT1A8	5.5 ± 0.48	550 ± 14	100	1.5 ± 0.17	110 ± 2.9	73
UGT1A10	0.87 ± 0.08	1100 ± 28	1260	0.96 ± 0.08	130 ± 3.1	140