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. 2021 Jun 17;13(6):899. doi: 10.3390/pharmaceutics13060899

Table 2.

Pharmacokinetic properties of uricosurics and hyperuricemic drugs discussed in this review. N/A, not available. 1 Assuming fu = 0.01 (if fu is not available, or the measured fu is <0.01). 2 Pharmacokinetic data from cynomolgus monkey. 3 Refers to the parent compound. 4 Steady-state trough concentration.

Drug/Compound MW Dose Cgut Cmax fu Cmax,u References
Uricosurics
Benzbromarone 424 100 mg 943 µM 7 µM 0.01 0.07 µM [91]
Probenecid 285 2000 mg 28.1 mM 520.7 µM 0.09 46.9 µM [70,92,93]
Lesinurad 404 200 mg 1.98 mM 29 µM 0.016 0.46 µM [94,95]
Verinurad 348 10 mg 115 µM 0.46 µM 0.02 0.0092 µM [96]
Dotinurad 358 4 mg 44.8 µM 1.2 µM 0.007 0.012 µM 1 [69]
Arhalofenate 416 600 mg 5.77 mM 337 µM N/A 3.37 µM 1 [97]
Fenofibrate 361 67 mg 742 µM 25.8 µM 0.01 0.236 µM [98]
Fenofibric acid 319 - - N/A N/A 0.81 µM [99]
Tranilast 327 200 mg 2.45 mM 129 µM N/A 1.29 µM 1 [100]
Losartan 423 50 mg 473 µM 0.60 µM 0.013 0.0078 µM [101]
Sulfinpyrazone 405 200 mg 1.98 mM 48.1 µM 0.017 0.82 µM [102]
Salicylate (high dose) 160 5200 mg 130 mM 1100 µM 0.25 275 µM [103,104]
Epaminurad (UR-1102, URC-102) 2 414 ~70 mg 676 µM 0.22 µM N/A 0.0022 µM 1 [105]
Hyperuricemic drugs
Bumetanide 364 1 mg 11.0 µM 0.8 µM 0.125 0.1 µM [72,106,107]
Furosemide 331 80 mg 970 µM 8–17 µM 0.041 0.697 µM [51,108]
Torasemide 348 200 mg 2.30 mM ~51.7 µM 0.01 0.517 µM [109,110]
Chlorothiazide 296 1000 mg 13.51 mM 120–240 µM >0.1 >24 µM [51]
Hydrochlorothiazide 298 100 mg 1342 µM 1.64 µM 0.33 0.54 µM [111]
Bendroflumethiazide 421 5 mg 47.5 µM 0.08–0.2 µM 0.05 4–10 nM [112,113]
Salicylate (low dose) 160 1000 mg 25 mM ~280 µM 0.25 ~70 µM [103,104]
Pyrazinoate (pyrazinamide metabolite) 124 3000 mg 3 - ≤150 µM 0.69 ≤103.5 µM [34,114]
Cyclosporine A 1202 300 mg 1.66 mM 1.5 µM 0.122 0.183 µM [115]
Favipiravir 157 2400 mg 61.1 mM 294 µM 4 0.46 135 µM 4 [116]
Favipiravir M1 173 1200 mg 3 - 87.9 µM 0.712 62.6 µM [117]