Table 5.

Transporter interaction profile of hyperuricemic agents. For each drug/transporter pair, results from different studies are separated by semicolons. All values are in µM unless noted otherwise. N/I, no inhibition; TS, trans-stimulation; (H)/(L), high/low affinity transport. The rules for highlighting in bold or bold and underlined are the same as in Table 3. Values in red were obtained using urate as a probe substrate. Abbreviations: Secr., secretion; Reabs., reabsorption.

Transporter	BCRP (Gut)	OAT1	OAT3	BCRP (Kidney)	MRP4	NPT4	URAT1	OAT4	OAT10	GLUT9
Role	Secr.	Secr.	Secr.	Secr.	Secr.	Secr.	Reabs.	Reabs.	Reabs.	Reabs.
Drug/Compound											References
Bumetanide	IC50 = ~100–1000	IC50 = 1.9 (rOat1);7.60	IC50 = 0.75	IC50 = ~100–1000	N/I; substrate; IC50 = ~ 10 -100	IC50 = 223.5		IC50 = 348			[51,71,72,147,148,149]
Furosemide	IC50 = 170	IC50 = 5.05; 18	IC50 = 51.1; 7.31	IC50 = 170	IC50 = 1.29	IC50 = 73.5	71.6% inhibition at 1 mM	IC50 = 44.5			[18,51,67,70,71,148]
Torasemide		Ki = 55.2	Ki = 89.9; TS of E3S transport				N/I	Ki = 47.0; TS of urate transport			[146]
Chlorothiazide	IC50 = 212.3	IC50 = 3.78	IC50 = 65.3	IC50 = 212.3	IC50 = 0.24nM (H)/10.4(L)	IC50 = 739.6		IC50 = 2632			[51,71,148,150]
Hydrochlorothiazide	N/I	IC50 = 126	IC50 = 213	N/I	IC50 = 1.9(H)/220 (L)			TS of urate uptake			[58,71,151]
Bendroflumethiazide		IC50 = 8 (mOat1)	IC50 = 21 (mOat3)								[152]
Salicylate (low dose)		IC50 = 1573.4; Ki = 341			IC50 = 2.1(H)/1547 (L)		TS of urate uptake				[34,71,75,103,104,125]
Pyrazinoate		IC50 = 582.6					N/I; TS of urate uptake				[18,34,104]
Cyclosporine A	IC50 = 4.6	N/I	N/I	IC50 = 4.6	N/I				TS of urate uptake		[59,73,153]
Favipiravir		30.9% inhibition at 800 µM	50.0% inhibition at 800 µM				65.7% inhibition at 800 µM				[145]
Favipiravir M1		45.4% inhibition at 300 µM	57.7% inhibition at 300 µM				31.0% inhibition at 300 µM; stimulation of urate uptake				[145]