Table 5 Summary of inhibition of CYP450 by (r)-SJ733 and (r)-SJ311
From: Selecting an anti-malarial clinical candidate from two potent dihydroisoquinolones
CYP | (r)-SJ733 | (r)-SJ311 | Probe substrate | Probe substrate metabolite |
|---|---|---|---|---|
CYP1A2 | − 5, 10.8%a | 5, 0.5% | Ethoxy-resorufin | Resorufin |
CYP2C9 | 34, 17% | 19, 15% | Diclofenac | 4′-Hydroxy diclofenac |
CYP2C19 | 5, 5% | 12, − 2% | S-mephenytoin | 4′-Hydroxy mephenytoin |
CYP2D6 | 7, 9% | 11, − 4% | Bufuralol | 1′-Hydroxy bufuralol |
CYP3A4 | 42, 33% | 54, 52% | Midazolam | 1′-Hydroxy midazolam |