Table 1.
Km and IC50 values of fluciclovine for specific drug transporters.
| Transporters | Km (mM) | IC50 (mM) |
|---|---|---|
| Efflux Transporters | ||
| P-gp | N.D. | 2.95 ± 2.56 |
| BCRP 1 | 1.34 ± 1.45 | N.D. |
| MRP4 1 | 15.3 ± 44.1 | 9.28 ± 1.90 |
| Uptake transporters | ||
| OAT1 2 | 258 ± 48.2 | 3.98 ± 1.77 |
| OAT3 3 | N.D. | |
| OCT2 3 | 275 ± 36.6 | 8.95 ± 1.96 |
| OATP1B1 4 | 401 ± 41.0 | 5.41 ± 2.49 |
| OATP1B3 5 | 238 ± 82.5 | N.D. |
All values represent the mean ± SD (n = 3–6). N.D.: Not determined within the concentration range used in this study. 1 Values at all points were not significant in comparison with those of control vesicles, but Km is shown because these data fit Michaelis–Menten kinetics; 2–5 The calculated Km values (μM) of the mock cells were 258 ± 127 (n = 6), 340 ± 43.1 (n = 3), 349 ± 40.0 (n = 3), and 340 ± 161 (n = 6). P-gp: P-glycoprotein; BCRP: breast cancer resistance protein; MRP4: multidrug resistance-associated protein 4; OAT1: organic anion transporter 1; OAT3: organic anion transporter 3; OCT2: organic cation transporter 2; OATP1B1: organic anion transporting polypeptide 1B1; OATP1B3: organic anion transporting polypeptide 1B3.