The formation of Almokalant metabolites in different in vitro models
| Model | [Almokalant] | M3 | M13 | M16 | M18a | M18b |
|---|---|---|---|---|---|---|
| μM | ||||||
| Microsomes (NADPH) | 20 | 4.53-a | 3.8 | 1.8 | N.D. | N.D. |
| Hepatocytes (biopsies, n = 4) | 250 | N.D. | N.D. | N.D. | 78 ± 363-b | 228 ± 64 |
| Hepatocytes (resection expt. A) | 100 | N.D. | N.D. | N.D. | 763-b | 196 |
| Hepatocytes (resection, expt. B) | 100 | N.D. | N.D. | N.D. | 13.1 | 56.9 |
| Tissue slices (expt. A) | 50 | N.L. | 1.33-c | 0.7 | N.D. | 9.5 |
| Tissue slices (expt. B) | 50 | N.D. | 3.2 | N.D. | 3.9 | 10.9 |