Determined in vitro inhibitory kinetic parameters of telithromycin vs. OATP1B1 and CYP3A4
| Type | Determined Inhibitory Kinetic Parameter Values | ||||||
|---|---|---|---|---|---|---|---|
| Expt 1 | Expt 2 | Expt 3 | Mean | S.D. | CV (%) | 95% CIa | |
| OATP1B1 Ki (IC50) (μM) | 13.7 | 11.3 | 11.1 | 12.0 | 1.45 | 12.1 | 8.40–15.6 |
| CYP3A4 Ki (μM) | 3.68 | 4.29 | 2.99 | 3.65 | 0.531 | 14.5 | 2.33–4.97 |
| CYP3A4 KI (μM) | 1.15 | 0.786 | 1.20 | 1.05 | 0.226 | 21.5 | 0.489–1.61 |
| CYP3A4 kinact (min−1 ) | 0.02492 | 0.03036 | 0.02790 | 0.02772 | 0.00272 | 9.8 | 0.02096–0.03448 |
Ki vs. the enzyme or transporter (for OATP1B1; assuming competitive inhibition, this equates to the IC50 value in the assay as the probe substrate concentration used is much lower than the Km value). CI, confidence interval; Expt, experiment.
↵a 95% CI was calculated by adding or subtracting the product of the t distribution value (4.303) and the value of the S.D. divided by the square root of the sample size from the determined mean value.