Table 2 Related parameters of the P-gp substrates used to establish linear regressions allowing the in vitro-in vivo extrapolation of diffusion and P-gp mediated efflux rates. Data were extracted from Collett and coworkers[38].
Drug Name | MW | LogP | Pappaba, c cm/s | Pappbaa, c cm/s | Vmax(P-gp)/Km(P-gp)a, c cm/s | Pdiffvitro cm/s | Pdiffvivob cm/s | PP-gp, vitro cm/s | RAUCcorrb | Ref |
|---|---|---|---|---|---|---|---|---|---|---|
Paclitaxel | 854 | 3 | 2.1 × 10-6 | 8.61 × 10-6 | 2.1 × 10-5 | 5.36 × 10-6 | 3.04 × 10-5 | 3.26 × 10-6 | 3.26 | |
Digoxin | 789 | 2.2 | 1.1 × 10-6 | 7.15 × 10-6 | 1.3 × 10-5 | 4.13 × 10-6 | 3.08 × 10-5 | 3.03 × 10-6 | 1.03 | |
Saquinavir | 670 | 3.8 | 2.2 × 10-6 | 1.21 × 10-5 | 2.3 × 10-5 | 7.15 × 10-6 | 2.77 × 10-5 | 4.95 × 10-6 | 6.5 | |
Topotecan | 421 | 0.8 | 1 × 10-6 | 3.5 × 10-6 | 1.2 × 10-5 | 2.25 × 10-6 | 2.35 × 10-5 | 1.25 × 10-6 | 2* | |
Verapamil | 454 | 4.7 | 1.5 × 10-5 | 1.5 × 10-5 | 0* | 1.5 × 10-5 | NA | 0* | NA | |
Talinolol | 363.5 | 2.9 | 1.5 × 10-6 | 1.5 × 10-5 | 1.5 × 10-5 | 6.0 × 10-6 | NA | 4.50 × 10-6 | NA | |
Rifampicin | 822 | 2.7 | 2.0 × 10-6 | 8.4 × 10-6 | 2.2 × 10-5 | 5.2 × 10-6 | NA | 3.20 × 10-6 | NA | |
UK 224,671 | 544 | 1.8 | 3.0 × 10-7 | 8.4 × 10-6 | 9.1 × 10-6 | 3.2 × 10-6 | 9.43 × 10-6 | 2.88 × 10-6 | 32** |