Table 2.
Interaction of drugs associated with nephrolithiasis with human renal OATs and other proximal tubular transporters. All values are in µM. T: transport demonstrated; n.t.: not transported; I: inhibition shown; n.i.: no inhibition; *: Km; ●: Ki; ◊: IC50; a: referral to unpublished data in [51].
| Substrate | OAT1 | OAT2 | OAT3 | OAT4 | Other Transporters | References | ||
|---|---|---|---|---|---|---|---|---|
| MRP2 | MRP4 | Additional Carriers | ||||||
| Cytostatics | ||||||||
| methotrexate (MTX) | *724; *554; n.t. | an.t.; T | *17.2; *10.9; *21.1 | *17.8 | *2500–3000; *250; *480 | *220; *220; *1300 | hOATP4C1: T | [10,13,19,51,52,103,129,131,132,133,134] |
| ß-Lactam Antibiotics | ||||||||
| Ceftriaxone | ●230 | ●6760 | ●4390 | ●2380 | T | PEPT1: n.i. | [29,32,33,36] | |
| Carboxyfluoroquinolones | ||||||||
| Ciprofloxacin | n.i. | I | MATE1: n.t.; ◊231; MATE2-K: n.t.; ◊98.7 | [135,136] | ||||
| Antivirals | ||||||||
| Acyclovir | *342 | n.i. | n.t.; I | n.i. | MATE1: *2640; MATE2-K: *4320 | [136,137] | ||