Table 2.

Kinetic analysis of OLZ glucuronidation in HLMs of varying UGT1A4 and UGT2B10 genotypes.

	OLZ-10-N-glucuronide isomer 1			OLZ-10-N-glucuronide isomer 2			OLZ-4’-N-glucuronide
HLM genotype	Vmax (pmol·min−1·mg−1)	KM (µM)	Vmax/KM (µl·min−1·mg−1)	Vmax (pmol·min−1·mg−1)	KM (µM)	Vmax/KM (µl·min−1·mg−1)	Vmax (pmol·min−1·mg−1)	KM (µM)	Vmax/KM (µl·min−1·mg−1)
UGT1A4(*1/*1)/ UGT2B10(*1/*1)*	94.0 ± 14	352 ± 59	0.28 ± 0.08	63 ± 23	311 ± 27	0.2 ± 0.07	82 ± 20	317 ± 39	0.26 ± 0.07
UGT1A4(*1/*3)/ UGT2B10(*1/*1)*	160 ± 14a	328 ± 33	0.50 ± 0.08b	73 ± 17	239 ± 22b	0.31 ± 0.08	70 ± 24d	263 ± 59	0.26 ± 0.04e
UGT1A4(*3/*3)/ UGT2B10(*1/*1)*	188 ± 47b	268 ± 41	0.70 ± 0.07c	106 ± 16	263 ± 86	0.42 ± 0.08	156 ± 18b	337 ± 37	0.46 ± 0.01c
UGT2B10(*1/*2)/ UGT1A4(*1/*1)**	56 ± 23d	302 ± 50	0.19 ± 0.08f	30 ± 14e	196 ± 54b	0.16 ± 0.09	47 ± 20e	602 ± 57a,e	0.08 ± 0.03b,g
UGT2B10(*2/*2)/ UGT1A4(*1/*1)**	69	273	0.25	41.5	271	0.15	37	796	0.047

^*Three HLM with the UGT1A4 (*1/*1) genotype, three HLM with the UGT1A4 (*1/*3) genotype, and two HLM with the UGT1A4 (*3/*3) genotype were examined in this analysis. Only HLM with the UGT2B10 (*1/*1) genotype was used to compare varying UGT1A4 genotypes. HLMs of each genotype were chosen at random.

^**Three HLM with the UGT2B10 (*1/*2) genotype and the single HLM with the UGT2B10 (*2/*2) genotype were examined in this analysis. Only HLM with the UGT1A4 (*1/*1) genotype were used to compare varying UGT2B10 genotypes.

^ap<0.005

^bp<0.05

^cp<0.01 versus the corresponding value for HLM with the UGT1A4 (*1/*1)/UGT2B10 (*1/*1) genotype.

^dp<0.05

^ep<0.01

^fp<0.005

^gp<1 versus the corresponding value for HLM with the UGT1A4 (*3/*3)/UGT2B10 (*1/*1) genotype.