TABLE 3

Dabigatran glucuronidation by human liver microsomes, inhibition experiments using inhibitors of various selectivity, and comparison with published data

A dabigatran concentration of 500 μM was used for inhibition experiments.

Inhibitor	UGT Inhibited	IC₅₀ or K_i^{^a}	Reference	IC₅₀ for Dabigatran Glucuronidation
		μM		μM
Oxazepam	2B7	31–63	Rios and Tephly, 2002	>200
Paclitaxel	1A1, 2B7	8.8 (1A1);	T. Ebner, unpublished data^{^b}	>200
		18.7 (2B7)
Niflumic acid	1A1, 1A9, 2B7	51.5 (1A1); 0.038 (1A9);	Mano et al., 2005, 2006, 2007	55.7
		83 (2B7)
Ritonavir	1A1, 1A3, 1A4	1.9 (1A1);	Zhang et al., 2005	10.4
		6.3 (1A3);
		2.0 (1A4)
Diclofenac	1A1, 1A9	112 (1A1);	Mano et al., 2005, 2006, 2007	155
		53.3, 24.2 (1A9);
		6.8 (2B7)
Ketoconazole	1A1, 1A9	3.3 (1A1)	Yong et al., 2005; Sampol et al., 1995	47.8
		31.9 (1A9);
		80 (2B7)
Hecogenin	1A4	1.5	Uchaipichat et al., 2006	>200
Codeine	2B7	3280	Macleod et al., 1992	>200
Sulfinpyrazone	1A1, 1A7, 1A9, 1A10	46 (1A1);	Uchaipichat et al., 2006	>200
		16 (1A7);
		11 (1A9);
		58 (1A10)

↵a IC₅₀ data are displayed in italics.
↵b IC₅₀ was assessed for inhibition of estradiol 2- and 17-glucuronidation, respectively, by human liver microsomes.