Table 4.
Relative inhibition potencies. The IC50 of each drug for a given transporter is compared with its IC50 for URAT1. For this calculation, the estimate IC50 = 2 × Ki was used when the IC50 was not available or 2 × Ki was lower than the available IC50. Values shown for each transporter are IC50transporter followed by the ratio IC50transporter/IC50URAT1). Relative inhibition values >1 indicate weaker inhibition, values <1 indicate stronger inhibition compared to URAT1. The rules for highlighting in bold or bold and underlined are the same as in Table 3. Abbreviations: Secr., secretion; Reabs., reabsorption.
| Transporter | OAT1 | OAT3 | BCRP (Kidney) | MRP4 | NPT1 | NPT4 | URAT1 | OAT4 | OAT10 | GLUT9 | |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Role | Secr. | Secr. | Secr. | Secr. | Secr. | Secr. | Reabs. | Reabs. | Reabs. | Reabs. | |
| Drug/Compound | References | ||||||||||
| Benzbromarone | 0.44 µM/4.2 | 0.22 µM/2.1 | 0.289 µM/2.8 | 0.104 µM/1.0 | 0.104 µM/1 | 3.19 µM/30.7 | >3 µM/>28.8 | ~100 µM/~961 | [69,71,94,105,119] | ||
| Probenecid | 4.66 µM/0.35 | 27.9 µM/2.11 | 132 µM/10.0 | 13.23 µM/1 | 15.54 µM/1.17 | [70,71,94] | |||||
| Lesinurad | 4.3 µM/1.22 | 1.07 µM/0.31 | 26.4 µM/7.54 | 3.53 µM/1 | 2.03 µM/0.58 | ~100 µM/~28.6 | [69,94,95] | ||||
| Verinurad | 4.6 µM/184 | 0.025 µM/1 | 5.9 µM/236 | [120] | |||||||
| Dotinurad | 4.08 µM/110 | 1.32 µM/35.5 | 0.0372 µM/1 | [69] | |||||||
| Arhalofenate | 92 µM/1 | 2.6 µM/0.028 | 53 µM/0.58 | [119] | |||||||
| Fenofibric acid | 4.4 µM/0.12 | 35.68 µM/1 | [121,122] | ||||||||
| Tranilast | ~15 µM/0.71 | 18.9 µM/0.90 | ~21 µM [68]/1 | ~22 µM/1.05 | ~31 µM/1.48 | 15.6 µM/0.75 | [68] | ||||
| Losartan | 12 µM/779 | 1.6 µM/104 | 1.5 µM/97.4 | 0.0154 µM/1 | 18 µM/1169 | [101] | |||||
| Sulfinpyrazone | IC50 = 0.16 µM (H)/0.047; 40 µM (L)/11.8 |
3.4 µM/1 | [71,120,124] | ||||||||
| Salicylate (high dose) | 682 µM/14.3 | 2.1 µM/0.088 | 23.9 µM/1 | [71,75,125] | |||||||
| Epaminurad | 14.4 µM/126 | 4.8 µM/42.1 | 0.114 µM/1 | [105] |