Table I.
Drug | Mol. type | BCS class | Log P | In vitro AUC FE ratio | Dog dose (mg) | Dog AUC FE ratio | Human dose (mg) | Human AUC FE ratio | Reference |
---|---|---|---|---|---|---|---|---|---|
BMS-A | Base | 2 | 2.36 | 1.04 | 30 | 0.9 | 40 | 1.17 | BMS |
BMS-B | Base | 4 | 3.87 | 3.29 | – | – | 300 | 3.17 | BMS |
BMS-C | Acid | 2 | 5.09 | 2.05 | 100 | 2.1 | 200 | 2.1 | BMS |
BMS-D | Base | 3 | 2.8 | 1.52 | 400 | 2.65 | 400 | 1.7 | BMS |
BMS-E | Base | 2 | 1.5 | 1.17 | 200 | 2.5 | 800 | 2.5 | BMS |
BMS-F | Acid | 3 | 0.59 | 0.7 | 20 | 0.7 | 20 | 0.69 | BMS |
BMS-G | Acid | 2 | 3.73 | 1.1 | 150 | 5.2 | 600 | 1.2 | BMS |
BMS-H | Base | 3 | −3.37 | 0.7 | 500 | 0.75 | 850 | 0.75 | BMS |
BMS-I | Base | 3 | 2.3 | 0.94 | 25 | 0.86 | 25 | 0.61 | BMS |
BMS-J | Base | 2 | 5.3 | 1.38 | 15 | 1.5 | 15 | 1.2 | BMS |
BMS-K | Base | 2 | 2.08 | 1.25 | – | – | 300 | 1.09 | BMS |
BMS-L | NI | 4 | 3.26 | 1.08 | – | – | 400 | 0.91 | BMS |
BMS-M | NI | 2 | 4.6 | 2.26 | 75 | 2.3 | 75 | 1.87 | BMS |
BMS-N | Base | 2 | 3.1 | 0.91 | 50 | 1.16 | 300 | 2.3 | BMS |
BMS-O | Base | 2 | 4.9 | 2.3 | 50 | 2.3 | 40 | 1.2 | BMS |
BMS-P | Base | 2 | 2.3 | 4.23 | 150 | 5.5 | 800 | 3.7 | BMS |
BMS-Q | Acid | 2 | 1 | – | 300 | 0.83 | 300 | 1.08 | BMS |
Ketoconazole | Base | 2 | 3.54 | 2.46 | – | – | 600 | 1.45 | (39) |
Ribavirin | Base | 3 | −2.6 | 1.2 | – | – | 200 | 1.42 | (40) |
Triclabendazole | Base | 2 | 6.34 | 10.01 | – | – | 600 | 3.7 | (26) |
Danazol | NI | 2 | 4.7 | 3.56 | – | – | 100 | 3 | (41) |
Celecoxib | Acid | 2 | 3 | – | 100 | 2.2 | 200 | 1.2 | (42) |
No value denotes the drug was not tested in that model. Molecule type: acid, base, or non-ionizable (NI)