Results from in vitro incubations of [14C]mavoglurant in recombinant human P450 enzymes and human liver microsomes (HLM)
| Incubation | Mavoglurant | M1/M2 | M3 | M7 | Other | Km | Vmax |
|---|---|---|---|---|---|---|---|
| % of total radioactivity in incubation | µM | pmol/(min·pmol P450 enzyme) | |||||
| Insect cell membrane (control) | 98.6 | ND | ND | ND | 1.40 | — | — |
| CYP1A2 | 98.1 | ND | 0.45 | ND | 1.45 | NA | NA |
| CYP2C8 | 97.0 | ND | ND | 1.66 | 1.34 | 17.1 | 5.06 |
| CYP2C9 | 98.2 | ND | ND | 1.21 | 0.59 | 2.49 | 1.15 |
| CYP2C19 | 93.9 | ND | 0.83 | 3.76 | 1.51 | 3.54 | 14.8 |
| CYP2D6 | 98.4 | ND | ND | 0.77 | 0.83 | NA | NA |
| CYP3A4 | 87.0 | 11.3 | ND | 0.44 | 1.23 | 7.78 | 84.1 |
| CYP1A1 | 95.7 | 0.54 | 3.22 | 0.51 | <0.10 | 0.80 | 45.7 |
| HLM | 87.7 | 10.0 | 0.11 | 1.60 | 0.59 | — | — |
NA, not analyzed; ND, not detected.