Efficacy and Safety of Diquafosol Ophthalmic Solution in Patients with Dry Eye Syndrome: A Japanese Phase 2 Clinical Trial

• Published in: Ophthalmology (Rochester, Minn.) Vol. 119; no. 10; pp. 1954 - 1960
• Main Authors: Matsumoto, Yukihiro, Ohashi, Yuichi, Watanabe, Hitoshi, Tsubota, Kazuo
• Format: Journal Article
• Language: English
• Published: New York, NY Elsevier Inc 01.10.2012; Elsevier
• Subjects: Administration, Topical; Biological and medical sciences; Cornea - metabolism; Double-Blind Method; Dry Eye Syndromes - drug therapy; Dry Eye Syndromes - metabolism; Female; Fluorophotometry; Humans; Japan; Male; Medical sciences; Middle Aged; Miscellaneous; Ophthalmic Solutions - administration & dosage; Ophthalmic Solutions - adverse effects; Ophthalmology; Polyphosphates - administration & dosage; Polyphosphates - adverse effects; Prospective Studies; Purinergic P2Y Receptor Agonists - administration & dosage; Purinergic P2Y Receptor Agonists - adverse effects; Tears - physiology; Treatment Outcome; Uracil Nucleotides - administration & dosage; Uracil Nucleotides - adverse effects; Japan; Human; Agonist; Toxicity; Diquafosol; Japanese; Eye; Dry eye syndrome; Eye disease; P2Y2 purinergic receptor; Phase II trial; Ophthalmology; Safety; Solution
• ISSN: 0161-6420; 1549-4713; 1549-4713
• DOI: 10.1016/j.ophtha.2012.04.010

To investigate the dose-dependent efficacy and safety of diquafosol ophthalmic solution for the treatment of dry eye syndrome. Randomized, double-masked, multicenter, parallel-group, placebo-controlled trial. A total of 286 Japanese patients with dry eye who were prescribed topical diquafosol (1%, n = 96; 3%, n = 96) or placebo ophthalmic solution (n = 94). After a washout period of 2 weeks, qualified subjects were randomized to receive a single drop of 1% or 3% diquafosol or placebo ophthalmic solutions 6 times per day for 6 weeks. The primary outcome measure was fluorescein corneal staining score assessment. The secondary outcome measures were Rose Bengal corneal and conjunctival staining scores, tear break-up time (BUT), and subjective symptom assessment. Safety measures were clinical blood and urine examination and recording of adverse events. Fluorescein corneal staining scores significantly improved with both 1% and 3% topical diquafosol compared with placebo at 4 weeks, respectively (P = 0.037, P = 0.002). There was a dose-dependent effect among the groups. Rose Bengal corneal and conjunctival staining scores also improved significantly with both 1% and 3% diquafosol compared with placebo (P = 0.007 and P = 0.004, respectively). Subjective dry eye symptom scores significantly improved with both diquafosol ophthalmic solutions (P ≤ 0.033), although there were no significant differences in BUT compared with placebo. No significant differences between the treatment groups were observed in relation to the occurrence of adverse events. Both 1% and 3% diquafosol ophthalmic solutions are considered effective and safe for the treatment of dry eye syndrome. Proprietary or commercial disclosure may be found after the references.