Table 1.
Prediction of the intestinal absorption and metabolic availability of tetrahydrocyclopropa[a]indene compounds
| Fabsa (%) | MFb mice (%) | MFb rat (%) | |
|---|---|---|---|
| S 50612 | 100 | 100 | 100 |
| S 51434 | 100 | 95 | 89 |
| S 49164 | 100 | 87 | 92 |
| S 50131 | 100 | 83 | 92 |
a
Fabs, prediction of the intestinal absorption based on permeability rates from the apical to the basal compartment of cultured Caco-2 cells. Percentages were calculated from a calibration curve obtained with reference compounds for which oral absorption in man was known (Yee, 1997). Values are means of duplicate wells from a single experiment.
b
MF, prediction of metabolic availability based on in vitro metabolic stability measurements with hepatic microsomes as a function of time. MF values were calculated from a single experiment as detailed previously (De Ceuninck et al., 2013).