Summary of the data for the potency and selectivity of etoricoxib in in vitro assays
| Assays | IC50 | |
|---|---|---|
| Etoricoxib | Indomethacin | |
| μM | ||
| PGE2 production by CHO (COX-2) cells | 0.079 ± 0.012 (n = 5) | 0.027 ± 0.006 (n = 12) |
| PGE2production by CHO (COX-1) cells | >50 (n = 2) | 0.018 ± 0.002 (n = 9) |
| TXB2production by Ca2+ ionophore-treated platelets | >100 (n = 4) | 0.002–0.007 |
| Purified human COX-2 | 5.0 ± 1.1 (n = 8) | 0.6 ± 0.1 (n = 16) |
| Purified human COX-2 with detergent | 4.1 ± 0.6 (n = 8) | 0.4 ± 0.1 (n = 16) |
| Purified human COX-1 (low substrate) | >100 (n = 2) | N.D. |
| Purified PGE2 production by U937 microsomes (low substrate) | 12.1 ± 2.5 (n = 4) | 0.0198 ± 0.0002 (n = 23) |
| Whole blood COX-2 | 1.1 ± 0.1 (n = 26) | 0.44 ± 0.07 (n = 34) |
| Whole blood COX-1 | 116 ± 18 (n = 12) | 0.19 ± 0.02 (n = 36) |
Values are means ± S.E. or range.
N.D., not determined.