Assessment of desloratadine as an inhibitor of P450 enzymes in pooled human liver microsomes (HLM)
P450 Enzyme | Substrate (Concentration) | Inhibition by 10 μM Desloratadine (% Activity Remaining) | |||
---|---|---|---|---|---|
Direct inhibition (Zero-min Preincubation) | TDI (30 min preincubation −NADPH) | MDI (30 min preincubation +NADPH) | Barecki et al., 2001a | ||
CYP1A2 | Phenacetin (40 μM) | 96.3 | 80.3 | 93.2 | 110b |
CYP2B6 | Bupropion (50 μM) | 51.8 | 59.5 | 59.6 | N.D. |
CYP2C8 | Paclitaxel (5 μM) | 98.9 | 117 | 100 | |
CYP2C9 | Diclofenac (6 μM) | 94.1 | 103 | 106 | 106 |
CYP2C19 | S-Mephenytoin (40 μM) | 89.3 | 91.9 | 87.2 | 112 |
CYP2D6 | Dextromethorphan (7.5 μM) | 68.4 | 67.0 | 78.1 | 86.3 |
CYP3A4/5 | Midazolam (3 μM) | 55.7 | 56.1 | 55.0 | 84.0c, 80.0d |