Advances in Corticosteroid Therapy for Ocular Inflammation: Loteprednol Etabonate

Table 1

Loteprednol etabonate: summary of randomized, controlled, clinical safety and efficacy studies in ocular Inflammatory diseases.

Ocular disease	Treatment duration and study treatments	Efficacy	Safety	Reference
	4 weeks LE 0.5% (𝑛=55) versus placebo (𝑛=55)	(i) Reduced papillary severity 1–4 (𝑃≤0.02 versus placebo); (ii) Investigators global assessment better (𝑃=0.017versus placebo)	No change in mean IOP in LE treatment group	[29]
Giant papillary conjunctivitis	6 weeks LE 0.5% (𝑛=111) versus placebo (𝑛=109)	(i) Reduced papillary severity at final visit (𝑃<0.001 versus placebo); (ii) Reduced itching at final visit (𝑃=0.001 versus placebo); (iii) Improved lens tolerance at final visit (𝑃=0.002 versus placebo)	↑ IOP (≥10 mm Hg): 𝑛=3 for LE; 𝑛=0 for placebo	[30]
	6 weeks LE 0.5% (𝑛=109) versus placebo (𝑛=110)	(i) Reduced papillary severity at final visit (𝑃=0.001 versus placebo); (ii) Reduced itching at final visit (𝑃<0.001 versus placebo); (iii) Improved lens tolerance at final visit (𝑃=0.053 versus placebo)	↑IOP (≥10 mm Hg): 7% versus 0%; 𝑛=8 for LE; 𝑛=0 for placebo	[31]
Prophylaxis of seasonal allergic conjunctivitis	6 weeks LE 0.5% (𝑛=145) versus placebo (𝑛=143)	(i) Reduced composite of itching and BCI (𝑃=0.001 versus placebo); (ii) Investigators global assessment better (𝑃<0.001 versus placebo)	↑ IOP (≥10 mm Hg): 𝑛=0for LE; 𝑛=2 for placebo	[32]
	6 weeks LE 0.2% (𝑛=66) versus placebo (𝑛=67)	(i) Reduced BCI, itching at 2 weeks (𝑃≤0.034 versus placebo); (ii) Investigator global assessment at week 2 better (𝑃<0.001 versus placebo)	No ↑ IOP (≥10 mm Hg) ≥1 AE: 68% versus 90% (𝑃=0.002)	[33]
Seasonal allergic conjunctivitis	6 weeks LE 0.2% (𝑛=67) versus placebo (𝑛=68)	(i) Reduced BCI, itching at 2 weeks (𝑃≤0.008versus placebo); (ii) Investigator global assessment at week 2 better (𝑃<0.001 versus placebo)	↑ IOP (≥10 mm Hg): 𝑛=1for LE; 𝑛=1 for placebo; No AE: 36% versus 19% (𝑃=0.035)	[34]
	2 weeks LE 0.2% (𝑛=151) versus olopatadine (𝑛=149)	(i) Reduced BCI, itching at week 2 in both groups (𝑃≤0.0006 in favour of LE)	No ↑ IOP (≥10 mm Hg) ≥1 AE: 2.0% versus 1.3% (𝑃=NS)	[35]
Anterior uveitis	6 weeks LE 0.5% (𝑛=36) versus prednisolone 1.0% (𝑛=34)	(i) Resolution of ACC (LOCF): 74% versus 88% (𝑃=NS); (ii) Resolution of flare (LOCF): 71% versus 81% (𝑃=NS); (iii) Resolution of pain (LOCF): 79% versus 81% (𝑃=NS)	↑ IOP (≥10 mm Hg): 𝑛=0 for LE; 𝑛=1 for prednisolone	[36]
	4 weeks LE 0.5% (𝑛=84) versus prednisolone 1.0% (𝑛=91)	(i) Resolution of ACC (LOCF): 72% versus 87% (𝑃=0.015 in favour of prednisolone); (ii) Resolution of flare (LOCF): 66% versus 82% (𝑃=0.017 in favour of prednisolone); (iii) Resolution of pain (LOCF): 90% versus 85% (𝑃=NS)	↑ IOP (≥10 mm Hg): 𝑛=1 for LE; 𝑛=6 for prednisolone	[36]
	Blepharokerato-conjunctivitis	2 weeks LE 0.5%/tobramycin 0.3% (𝑛=136) versus dexamethasone 0.1%/tobramycin 0.3% (𝑛=137)	(i) Improvement from baseline in composite signs and symptoms severity at day 15 in both groups; (ii) LE/T noninferior to DM/T in reduced composite signs and symptoms at day 15 (−15.2 [7.3] versus −15.6 [7.7], 𝑃=NS); (iii) Investigator global assessment: 43.6% versus 40.9% cured (𝑃=NS)	↑ IOP (≥10 mm Hg): 𝑛=0 for LE/T; 𝑛=1 for DM/T Mean IOP increase at day 15: −0.1 mm Hg versus 1.0 mm Hg (𝑃=0.0091) ≥1 AE: 2.9% versus 6.5% (𝑃=NS)	[43]
2 weeks LE 0.5%/tobramycin 0.03% (𝑛=178) versus dexamethasone 0.1%/tobramycin 0.3% (𝑛=176)		(i) Improvement from baseline in composite signs and symptoms severity at day 15 in both groups (𝑃<0.0001 versus baseline); (ii) LE/T noninferior to DM/T in reduced composite signs and symptoms at day 15 (−11.6 [4.6] versus −12.4 [4.7], 𝑃=NS)	↑ IOP (≥10 mm Hg): 𝑛=6 for LE/T; 𝑛=13 for DM/T; Mean IOP increase at day 15: 1.33 mm Hg versus 2.43 mm Hg (𝑃=0.0039) ≥1 AE: 13.0% versus 23.2%	[44]
Keratoconjunctivitis sicca		4 weeks 0.5% LE (𝑛=32) versus placebo (𝑛=34)	(i) Reduced hyperaemia at week 2 and week 4 (𝑃≤0.0473 versus placebo); (ii) Subset analysis in patients with moderate-to-severe inflammation at baseline; (iii) Reduced central corneal staining, nasal bulbar conjunctival hyperaemia, and lid margin injection at some visits (𝑃<0.05 versus placebo)	No ↑IOP (≥10 mm Hg); No significant change in mean IOP ≥1 AE: 16.7% versus 23.5%	[38]

LE: loteprednol etabonate, IOP: intraocular pressure, ACC: anterior chamber cells, AE: adverse event, BCI: bulbar conjunctival injection, LOCF: last observation carried forward, NS: not significant.