Novel dry eye drug found safe, effective

This phase 3 study found that 2% rebamipide ophthalmic suspension was effective at improving both the objective signs and subjective symptoms of dry eye without adverse events.

The authors compared the efficacy of 2% rebamipide ophthalmic suspension, a quinolinone derivative used in Japan as an oral therapeutic for gastric mucosal disorders under the trade name Mucosta, with that of 0.1% sodium hyaluronate ophthalmic solution in 108 patients with dry eye. Sodium hyaluronate was selected as the active control because it is an indicated treatment for keratoconjunctival disorder accompanying dry eye in Japan and has demonstrated clinical efficacy. After a two-week screening period, patients were randomized to rebamipide or sodium hyaluronate, administered as one drop in each eye, four or six times daily, respectively, for four weeks.

Mean change from baseline in fluorescein corneal staining scores indicated significant improvement and verified noninferiority of rebamipide. Lissamine green conjunctival staining verified the superiority of rebamipide to sodium hyaluronate.

Schirmer's test and TBUT values were comparable between the two groups. For two dry eye-related ocular symptoms-foreign body sensation and eye pain-rebamipide showed significant improvements over sodium hyaluronate. Patients had a significantly more favorable impression of rebamipide than sodium hyaluronate; 64.5 percent rated treatment as improved or markedly improved versus 34.7 percent, respectively. No serious adverse events were observed.

In a previous study, when rebamipide was instilled in rabbit eyes, it increased production of mucin-like substances and periodic acid-Schiff-positive cells. A recent study also reported a significant increase in a mucin-like glycoprotein and MUC1 and MUC4 gene expression after human corneal epithelial cells were incubated with rebamipide.

The results of the current study suggest that use of rebamipide may lead to improved treatment of corneal and conjunctival epithelial damage and improvement in symptoms in patients with dry eye. Rebamipide's efficacy and tolerability make it a potentially useful treatment option for dry eye.