Still only available abroad (like Japan: see below), Rebamipide show promise in helping relieve patient’s dry eye symptoms.

We are investigating how to formulate a drop from the FDA approved systemic medication via the NIH currently.

Best regards,
Sandra Lora Cremers, MD, FACS

Rebamipide ophthalmic suspension for the treatment of dry eye syndrome: a critical appraisal

Review

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Authors: Kashima T, Itakura H, Akiyama H, Kishi S

Published Date May 2014 Volume 2014:8 Pages 1003 – 1010

DOI: http://dx.doi.org/10.2147/OPTH.S40798

Received:	03 January 2014
Accepted:	08 March 2014
Published:	30 May 2014

Tomoyuki Kashima,¹ Hirotaka Itakura,^1,2 Hideo Akiyama,¹ Shoji Kishi¹

¹Department of Ophthalmology, Gunma University, School of Medicine, Maebashi, Gunma, Japan; ²Department of Ophthalmology, Maebashi Red Cross Hospital, Maebashi, Gunma, Japan

Abstract: Rebamipide was initially developed and approved for use in treating gastric ulcers and lesions associated with gastritis. Discovery of its ability to increase gastric mucin led to investigations of its effect on ocular surface mucin and the subsequent development for use in dry eye patients. Investigations have confirmed that rebamipide increases corneal and conjunctival mucin-like substances along with improving corneal and conjunctival injury. Clinically, rebamipide ophthalmic suspensions can effectively treat tear deficiency and mucin-caused corneal epithelial damage, and can restore the microstructure responsible for tear stability. Topical rebamipide has also been shown to be effective in treating other ocular surface disorders such as lagophthalmos, lid wiper epitheliopathy, and persistent corneal erosion. Rebamipide’s ability to modify epithelial cell function, improve tear stability, and suppress inflammation in the absence of any known major side effects suggest that it may be a beneficial first drug of choice for severe dry eye treatment and other ocular surface disorders. This review summarizes the history and development of this innovative dry eye treatment from its initial use as an effective stomach medication to its current use in the treatment of dry eye in Japan.

Keywords: quinolinone derivative, tear deficiency, ocular surface disorder, mucin secretion, Mucosta

2014 Apr;157(4):807-812.e2. doi: 10.1016/j.ajo.2013.12.027. Epub 2014 Jan 9.

Topical rebamipide treatment for superior limbic keratoconjunctivitis in patients with thyroid eye disease.

Takahashi Y1, Ichinose A2, Kakizaki H3.

Author information

1Department of Ophthalmology, Aichi Medical University, Nagakute, Aichi, Japan.
2Department of Plastic Surgery, Kobe University School of Medicine, Kobe, Hyogo, Japan.
3Department of Ophthalmology, Aichi Medical University, Nagakute, Aichi, Japan. Electronic address: cosme@d1.dion.ne.jp.

Abstract

PURPOSE:

To evaluate efficacy of topical rebamipide for superior limbic keratoconjunctivitis (SLK) in patients with thyroid eye disease.

DESIGN:

Retrospective, observational case series.

METHODS:

Thirty-three eyes from 20 thyroid eye disease patients with SLK who received topical rebamipide (Mucosta ophthalmic suspension unit dose 2%; Otsuka Pharmaceutical Co, Ltd; chemical name, (2RS)-2-(4-chlorobenzoylamino)-3-(2-oxo-1, 2-dihydroquinolin-4-yl) propanoic acid) were included. The following items were evaluated before and 4 weeks after the start of treatments: presence or absence of SLK, rose bengal staining score, area and density classification of fluorescein staining, Schirmer test I results (without topical anesthesia), tear film break-up time, Hertel exophthalmometry values, and margin reflex distances 1 and 2.

RESULTS:

Twenty-eight eyes showed complete disappearance of SLK after treatment (84.8%; P < .001). The other 5 eyes (15.2%) demonstrated significant improvement, but had residual punctate rose bengal staining and fluorescein staining near the superior corneal limbus. All 5 eyes exhibited at least 1 of the following findings: proptosis of more than 17.7 mm and upper or lower eyelid retractions or both. Incidence of upper eyelid retraction was significantly higher in eyes with SLK than in those without SLK at the 4-week follow-up (P = .021). The severity of rose bengal staining and fluorescein staining improved significantly after treatment (P < .001). Although the Schirmer test results remained constant before and after the treatment (P = .212), tear film break-up time increased significantly in the posttherapeutic state (P = .009). No serious adverse events were reported.

CONCLUSIONS:

Topical rebamipide improved SLK in patients with thyroid eye disease, suggesting a first-line treatment in such patients.