TABLE 1.
Inhibition constants (µM) of telmisartan and bosentan against transporters involved in the hepatic uptake and efflux of TCA
| Clearance | Transporter | Telmisartan | Reference | Bosentan | Reference |
|---|---|---|---|---|---|
| CLUptake | NTCP | 60 (Ki) | (Dong et al., 2014) | 18 (Ki) | (Leslie et al., 2007; Lepist et al., 2014) |
| 36 (IC50) | |||||
| OATP1B1 | 0.44 (Ki) | (Hirano et al., 2006) | 18a | ||
| CLBile | BSEP | 16–16.2 (IC50) | (Morgan et al., 2013; Lai, 2014) | 23–42 (IC50) | (Morgan et al., 2013) (Lepist et al., 2014) |
| CLBL | MRP4 | 11–36 (IC50) | (Sato et al., 2008) | 22 (IC50) | (Morgan et al., 2013) |
| (Morgan et al., 2013) | |||||
| MRP3 | 60 (IC50) | (Morgan et al., 2013) | 42 (IC50) | (Morgan et al., 2013) |
a
Not available and therefore assumed to be the same as NTCP.