TABLE 4

Description of bias (gmfe) and percentage within 1.5-fold of unity for predictions of the FG for either total set of 25 drugs or for a subset of 11 drugs for which in vivo FG < 0.5

Different permeability approaches were used as follows: 1, Papp (A-B) data from Caco-2 (data in parentheses: MDCK-MDR1); 2, Peff data from correlation to Papp (A-B) from Caco-2 (data in parentheses: MDCK-MDR1); 3, Peff data from correlation to Papp (A-B) from Caco-2 (data in parentheses: MDCK-MDR1) calibrated for midazolam QGut; and 4, Peff data from correlation to in silico data (data in parentheses: calibrated for midazolam QGut).

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Total set of drugs (n = 25)
    <1.5-Fold (%)64 (60)52 (60)56 (60)44 (44)
    gmfe1.82 (1.74)2.29 (2.14)1.89 (1.89)3.93 (3.34)
Drugs with in vivo FG < 0.5 (n = 11)
    <1.5-Fold (%)27 (18)18 (27)9 (18)18 (9)
    gmfe2.89 (2.67)4.15 (3.65)2.82 (2.74)9.55 (7.35)