Table 1.
Effect of transporter inhibition on drug transfer across perfused term human placentae.
| Transporter | Drug (concentration) | Inhibitor (concentration) | Fold change in maternal-to-fetal transfer in inhibitor-treated vs. control placentae(P)a | Fold change in fetal-to- maternal transfer in inhibitor-treated vs. control placentae (P)a | Reference |
|---|---|---|---|---|---|
| P-gp | Saquinavir (6.7 μg/mL) | PSC833 (2.4 μg/mL) | 3.5 (<0.01) | 0.7 (>0.05) | Mölsä et al. (2005) |
| GF120918 (0.6 μg/mL) | 3.0 (<0.01) | ND | |||
| Indinavir (7.6 μg/mL) | PSC833 (1.2 μg/mL) | 1.5 (<0.05) | ND | Sudhakaran et al. (2008) | |
| Ritonavir (0.22 μg/mL) | 1.1 (>0.05) | ND | |||
| Lopinavir (6 μg/mL) | CsA (12.0 μg/mL) | 10.3 (<0.05) | ND | Ceccaldi et al. (2009) | |
| Talinolol (0.29 μg/mL) | Verapamilb (13.6 μg/mL) | 1.2 (<0.05) | ND | May et al. (2008) | |
| PSC833 (2.2 μg/mL) | 1.0 (>0.05) | ND | |||
| Paclitaxel (0.085 μg/mL) | GF120918 (0.6 μg/mL) | 1.7 (<0.01) | ND | Nanovskaya et al. (2005) | |
| Methadone (0.2 μg/mL) | GF120918 (0.6 μg/mL) | 1.3 (<0.01) | ND | ||
| MRPs | Talinolol (0.29 μg/mL) | Probenecidc (2.9 μg/mL) | 1.2 (<0.05) | ND | May et al. (2008) |
| Saquinavir (6.7 μg/mL) | MK-571 (26.9 μg/mL) | ND | 0.9 (>0.05) | Rahi et al. (2009) | |
| Probenecidc (14.3 μg/mL) | ND | 0.8 (>0.05) | |||
| OCTs | Metformin (2.0 μg/mL) | Cimetidine (100 μg/mL) | 1.3 (>0.05) | 1.3 (>0.05) | Tertti et al. (2010) |
The methodology for calculation of maternal-to-fetal and fetal-to-maternal transfer varied across studies. aValues are normalized to changes in the transfer of markers for passive diffusion. bAlso an MRP1 and OATPs inhibitor. cAlso an OATPs inhibitor. ND, not determined.