Pathways | Human Livers | Km | Vmax | CIint |
---|---|---|---|---|
μM | nmol/h/mg protein | ml/h/mg protein | ||
All | GGM002 | 22.6 | 243.8 | 10.8 |
HL-44A | 18.2 | 128.3 | 7.1 | |
HL-46A | 19.6 | 172.0 | 8.8 | |
mean ± S.D. | 20.1 ± 2.2 | 181.4 ± 58.3 | 8.9 ± 1.9 | |
Side-chain oxidation | GGM002 | 12.8 | 19.9 | 1.6 |
OL+CA+DOL | HL-44A | 5.9 | 16.8 | 2.8 |
HL-46A | 14.9 | 9.7 | 0.7 | |
mean ± S.D. | 11.2 ± 4.7 | 15.5 ± 5.2 | 1.7 ± 1.1 | |
N-Demethylation | GGM002 | 17.0 | 72.4 | 4.3 |
D+DOL+D-DHDs | HL-44A | 12.1 | 32.6 | 2.7 |
HL-46A | 16.7 | 51.0 | 3.1 | |
mean ± S.D. | 15.3 ± 2.7 | 52.0 ± 19.9 | 3.4 ± 0.8 | |
Deamination | GGM002 | 24.6 | 96.1 | 3.9 |
NAL+NM+NA | HL-44A | 33.2 | 60.1 | 1.8 |
HL-46A | 25.6 | 89.8 | 3.5 | |
mean ± S.D. | 27.8 ± 4.7 | 82.0 ± 19.2 | 3.1 ± 1.1 | |
Dihydrodiol formation | GGM002 | 3.6 | 13.8 | 3.9 |
DHDs+D-DHDs | HL-44A | 5.8 | 8.6 | 1.5 |
HL-46A | 3.8 | 6.9 | 1.8 | |
mean ± S.D. | 4.4 ± 1.2 | 9.8 ± 3.6 | 2.4 ± 1.3 |
[14C]Terbinafine (2–220 μM) metabolite formation was investigated by three different human liver microsomal preparations.