title: Diquafosol ophthalmic solution for dry eye treatment.
abstract: BACKGROUND
  There has been rapid progress in our understanding of dry eye pathogenesis, as well as the development of improved diagnostic clinical tests. Various types of dry eye treatment drugs have been developed. This review summarizes the basic and clinical research carried out in the development of diquafosol for ophthalmic use.
  
  
  RESULTS
  Diquafosol is a dinucleotide, purinoreceptor P2Y(2) receptor agonist. Basic pharmacological studies have shown that it acts on P2Y(2) receptors at the ocular surface, to promote tear and mucin secretion via elevated intracellular Ca(2+) concentrations. Diquafosol also improves tear and mucin secretion in experimental dry eye models. Based on the results of laboratory experiments, the authors conducted a series of clinical studies in patients with dry eye disease. Diquafosol was effective in the treatment of dry eye disease at an optimal dose of 3% six times a day. In comparison to commercially available 0.1% sodium hyaluronate ophthalmic solution, 3% diquafosol ophthalmic solution showed non-inferiority in improving corneal fluorescein staining scores and superiority in improving keratoconjunctival Rose Bengal staining scores.
  
  
  CONCLUSIONS
  Diquafosol ophthalmic solution has a novel mechanism of action that is characterized by its stimulatory effects on tear and mucin secretion. This drug has the potential to be effective in patients with tear film instability and short break-up time type of dry eye, which are essential factors in dry eye pathogenesis.
authors: Research and Development Division, Santen Pharmaceutical Co., Ltd., 8916-16, Takayama-cho, Ikoma-shi, Nara 630-0101, Japan. nakamuram@santen.co.jp
authors: Masatsugu
authors: M
authors: Nakamura
authors: Takahiro
authors: T
authors: Imanaka
authors: Asuka
authors: A
authors: Sakamoto
mesh_terms: D015352:Dry Eye Syndromes / Q000188:drug therapy*; D006801:Humans; D009077:Mucins / Q000378:metabolism; D009883:Ophthalmic Solutions / Q000627:therapeutic use*; D011122:Polyphosphates / Q000627:therapeutic use*; D058912:Purinergic P2Y Receptor Agonists / Q000627:therapeutic use*; D013666:Tears / Q000378:metabolism; D016896:Treatment Outcome; D014500:Uracil Nucleotides / Q000627:therapeutic use*
chemical_list: D009077:Mucins; D009883:Ophthalmic Solutions; D011122:Polyphosphates; D058912:Purinergic P2Y Receptor Agonists; D014500:Uracil Nucleotides; C403315:diquafosol