Compound | P-gP Efflux Ratioa | BCRP Efflux Ratioa | P-gp Substrate | BCRP Substrate | ||
---|---|---|---|---|---|---|
No Inhibitor | + GF120918 | No Inhibitor | + GF120918 | |||
Dabrafenib | 36 | 1.0 | 3.6 | 1.3 | Yes | Yes |
Hydroxy-Dabrafenib | 120 | 1.0 | 13 | 1.3 | Yes | Yes |
Carboxy-Dabrafenib | 1.8 | 1.3 | 0.7 | 1.1 | No | No |
Desmethyl-Dabrafenib | 21 | 0.9 | 6.6 | 1.3 | Yes | Yes |
↵a Efflux ratio equals Papp [B→A])/Papp [A→B]. A compound is considered a substrate when the efflux ratio is >2 in the absence of GF120918 and close to 1 in the presence of GF120918.