TABLE 3.
Effect of doravirine on the activity of human uptake and efflux transportersa
| Transporter | Substrate (concn, μM) | Maximum concn of doravirine tested (μM) | IC50 of doravirine (μM)b |
|---|---|---|---|
| BCRP | Methotrexate (10) | 75 | 51 + 4 |
| P-gp | Digoxin (0.1) | 100 | >100 (3) |
| OATP1B1 | Pitavastatin (0.1) | 75 | 39 + 2 |
| OATP1B3 | Bromosulfophthalein (0.1) | 75 | 31 + 4 |
| BSEP | Taurochloric acid (1) | 50 | >50 (0) |
| OAT1 | Cidofovir (1) | 75 | >75 (13) |
| OAT3 | Estrone sulfate (1) | 75 | 16.0 + 0.7 |
| OCT2 | Metformin (10) | 75 | 67 + 9 |
| MATE1 | Metformin (5) | 50 | >50 (28) |
| MATE2K | Metformin (5) | 50 | >50 (39) |
a
BCRP, breast cancer resistance protein; BSEP, bile salt extrusion pump; IC50, half-maximal inhibitory concentration; MATE, multidrug and toxin extrusion protein; OAT, organic anion transporter; OATP, organic anion transporting polypeptide; OCT, organic cation transporter; P-gp, P-glycoprotein.
b
IC50 values are expressed as mean ± SEM. Values in parentheses represent the mean percent inhibition at the maximal concentration tested when the IC50 was above it.