Transcellular transport of lemborexant and its metabolites via P-gp and BCRP
| Compound | Corrected Flux Ratio | |||
|---|---|---|---|---|
| P-gp | BCRP | |||
| – | + | – | + | |
| Lemborexant | 1.47 | 1.16 | 1.28 | 1.21 |
| M4 | 16.3 | 2.32 | 1.42 | 1.21 |
| M9 | 2.86 | 1.19 | 1.04 | 1.14 |
| M10 | 4.41 | 1.22 | 0.94 | 0.99 |
Values represent corrected flux ratios in the absence (–) and presence (+) of a typical inhibitor of P-gp (30 µmol/l verapamil) or BCRP (50 nmol/l Ko143).