Permeability and transporter data of PF-06282999 in Caco-2, MDCKII-LE, and MDCKII-MDR1 cell monolayers
| Compound | A-to-B Papp | B-to-A Papp | Efflux Ratio | Fold Change from A to B at pH 7.4 |
|---|---|---|---|---|
| Caco-2 | × 10−6 cm/s | |||
| PF-06282999 (pH 7.4) | 2.7 | 10 | 3.8 | |
| PF-06282999 (pH 6.0) | 2.7 | 1 | ||
| PF-06282999 (pH 7.4, Ca2+-free) | 12 | 4.4 | ||
| PF-06282999 (pH 7.4) + MDR1 inhibitors | 2.9 | 7.6 | 2.6 | 1.1 |
| MDCKII-LE | ||||
| PF-06282999 (pH 7.4) | 2.2 | |||
| MDCKII-MDR1 | ||||
| PF-06282999 (pH 7.4) | 0.6 | 2.1 | 3.3 | |
A, apical; B, basolateral.