Inhibition of human OATP1B1- and OATP1B1*15-mediated transport of [3H]-E217β-G and [3H]-rosuvastatin by selected oral antidiabetic drugs
| Class | Drug | Inhibition of [3H]-E217β-G Uptake | Inhibition of [3H]-Rosuvastatin Uptake | ||||
|---|---|---|---|---|---|---|---|
| OATP1B1 | OATP1B1*15 | OATP1B1 | |||||
| IC50 | 95% CI | IC50 | 95% CI | IC50 | 95% CI | ||
| μM | μM | μM | |||||
| Sulfonylurea | Glyburide | 2.99 | 1.88–7.56 | 2.60 | 1.22–5.53 | 1.77 | 1.50–2.10 |
| Glipizide | ∼45.3 | 0.72–2845a | ∼48.4 | 0.59–3948a | 110 | 54.4–224 | |
| Gliclazide | >100 | na | >100 | na | 580 | 335–1005 | |
| Glimepiride | 3.55 | 1.60–7.89 | 6.24 | 2.06–18.9 | 3.62 | 2.79–4.69 | |
| Tolbutamide | >100 | na | >100 | na | 368 | 168–806 | |
| Thiazolidinedione | Troglitazone | 2.50 | 1.33–4.70 | 3.08 | 1.36–6.98 | 2.84 | 2.23–3.63 |
| Pioglitazone | 5.09 | 1.89–13.7 | 5.32 | 1.34–21.2 | 32.2 | 17.4–59.8 | |
| Biguanide | Metformin | >100 | na | >100 | na | >1000 | na |
CI, confidence interval; E217β-G, estradiol 17β-d-glucuronide; na, not applicable; OATP, organic anion-transporting polypeptide.
↵a 95% confidence interval is very wide due to incomplete and nonsigmoidal fitting of the curve; IC50 value is estimated (although >50% inhibition is observed at highest measured concentration of 100 µM).