P2Y₂ receptor agonists for the treatment of dry eye disease: a review

Figures & data

Table 1 Key clinical trials evaluating topical diquafosol therapy for dry eye disease

Study	Year of publication	Study design	Number of patients (n), study arms	Predominant type of dry eye studied	Duration (weeks)	Results
Tauber et al^Citation34	2004	Randomized controlled trial	n=527 Three arms: 1) 1% diquafosol 2) 2% diquafosol 3) placebo	ADDE	24	Schirmer scores and corneal fluorescein staining significantly improved with both 1% and 2% diquafosol. Minor improvement in “clearing of foreign body sensation” on secondary (but not primary) analysis.
Matsumoto et al^Citation33	2012	Randomized controlled trial	n=286 Three arms: 1) 1% diquafosol 2) 3% diquafosol 3) placebo	ADDE	6	Corneal and conjunctival staining scores significantly improved with both 1% and 3% topical diquafosol with a dose-dependent effect. eleven ocular symptoms were assessed. Only one (“dry eye sensation”) improved with diquafosol.
Takamura et al^Citation35	2012	Randomized controlled trial	n=286 Two arms: 1) 3% diquafosol 2) 0.1% sodium hyaluronate	ADDE	4	Mean fluorescein staining scores and TBUT improved for both groups. No inferiority or superiority detected between groups. Rose bengal staining improved for both groups, with diquafosol superior to hyaluronate. Eleven ocular symptoms were assessed; superiority of diquafosol was demonstrated for one (“heaviness”).
Kamiya et al^Citation36	2012	Prospective, consecutive interventional case series	n=32 (64 eyes) For each patient: 1) one eye served as treatment group (sodium hyaluronate and diquafosol) 2) the other eye served as control (sodium hyaluronate)	ADDE insufficiently responsive to sodium hyaluronate monotherapy	4	Diquafosol eyes showed improvement in TBUT and corneal staining but not Schirmer test. Twelve symptoms were measured. Three (“dry eye sensation, pain, and foreign body sensation”) improved in diquafosol eyes.

Abbreviations: ADDE, aqueous tear-deficient dry eye; TBUT, tear film break-up time.

TauberJDavittWFBokoskyJEDouble-masked, placebo-controlled safety and efficacy trial of diquafosol tetrasodium (INS365) ophthalmic solution for the treatment of dry eyeCornea200423878479215502479

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MatsumotoYOhashiYWatanabeHTsubotaKDiquafosol Ophthalmic Solution Phase 2 Study GEfficacy and safety of diquafosol ophthalmic solution in patients with dry eye syndrome: a Japanese phase 2 clinical trialOphthalmology2012119101954196022739038

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TakamuraETsubotaKWatanabeHOhashiYDiquafosol Ophthalmic Solution Phase 3 Study GA randomised, double-masked comparison study of diquafosol versus sodium hyaluronate ophthalmic solutions in dry eye patientsBr J Ophthalmol201296101310131522914501

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KamiyaKNakanishiMIshiiRClinical evaluation of the additive effect of diquafosol tetrasodium on sodium hyaluronate monotherapy in patients with dry eye syndrome: a prospective, randomized, multicenter studyEye201226101363136822878452

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