Key trial characteristics and IOP and pharmacological effects of orally administered drugs in clinical trials to reduce cortisol levels
| Drug name (reference) | Drug type | Design and regimen | Effect on IOP (mm Hg) (n) (mean±SD or 95% CI) | Primary pharmacological effect (systemically) |
| Metpyrapone14 | Inhibitor of adrenal cortisol biosynthesis (CYP11B1) | Two-way cross-over, single administration | −4.9±3.0 (active drug) (14) −2.6±2.2 (placebo) only highest effect for statistically significant time points shown | Up to about 80% plasma cortisol reduction from baseline |
| Carbenoxolone8 | 11βHSD1/2 inhibitor | Two-way cross-over, t.i.d. for 4 days | −2.2 (active drug) (20) −0.8 (placebo) p=0.0003 | Urinary THF/THE ratio:decrease from 1.09±0.25 to 0.78±0.58 (n=7) in healthy volunteers, statistically significant |
| AZD401716 | 11βHSD1 inhibitor | Parallel groups, twice daily or four times a day for 4 weeks | −2.6 (−3.8 to −1.3) (twice daily active drug) (19) −1.9 (−3.3 to −0.6) (twice daily placebo) (16) +0.1 (−4.8 to 4.9) (four times daily placebo) (6) | No data available |
| RO5093151 (this study) | 11βHSD1 inhibitor | Parallel groups, twice daily for 7 days | −2.7 (−4.2 to −1.2) (active drug) (20) −2.9 (−5.9 to 0.1) (placebo) (5) (worse eye) | Urinary THF/THE ratio decreased from 0.90±0.34 (day 1 baseline) to 0.18±0.32 (day 7 trough) |
11βHSD1, 11β-hydroxysteroid-dehydrogenase type 1; IOP, intraocularpressure; THE, tetrahydrocortisone; THF, tetrahydrocortisol.