Table 1.

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.