Pharmacokinetic evaluation of diquafosol tetrasodium for the treatment of Sjögren's syndrome

Expert Opin Drug Metab Toxicol. 2014 Jun;10(6):905-13. doi: 10.1517/17425255.2014.915026. Epub 2014 May 6.


Introduction: Dry eye is a multifactorial disease of the ocular surface causing ocular discomfort and visual impairment for the patient. A variety of topical and systemic drugs are available to treat dry eye. Conventional treatments are limited to tear supplementation or improvement of ocular surface inflammation by the use of corticosteroids or cyclosporine A. Treatment of severe dry eye associated with Sjögren's syndrome (SS) is even more challenging and is designed to improve the quality and quantity of tear fluid. Diquafosol tetrasodium , a P2Y2 purinergic receptor agonist, acts via a novel mechanism by activating P2Y2 receptors of the ocular surface.

Areas covered: The aim of this review is to summarize the pharmacokinetics, and pharmacological and clinical data of 3% diquafosol tetrasodium ophthalmic solution in patients with dry eye, particularly SS. The mechanisms of impaired ocular surface due to severe dry eye, as defined by the International Dry Eye Workshop, are analyzed.

Expert opinion: Diquafosol tetrasodium provides a novel mode of action in dry eye syndrome, including SS, by stimulating the quantity and quality of tear fluid secretion via various mechanisms. In clinical trials, 3% Diquafosol tetrasodium ophthalmic solution demonstrated a good safety profile and exhibited efficacy with clinical improvement of the ocular surface in dry eye including SS.

Keywords: Sjögren's syndrome; clinical studies; clinical trial; diquafosol tetrasodium; dry eye disease; tear film.

Publication types

  • Review

MeSH terms

  • Humans
  • Ophthalmic Solutions
  • Polyphosphates / pharmacokinetics*
  • Polyphosphates / therapeutic use
  • Purinergic P2Y Receptor Agonists / pharmacokinetics*
  • Purinergic P2Y Receptor Agonists / therapeutic use
  • Sjogren's Syndrome / complications
  • Sjogren's Syndrome / drug therapy*
  • Sjogren's Syndrome / metabolism
  • Uracil Nucleotides / pharmacokinetics*
  • Uracil Nucleotides / therapeutic use
  • Xerophthalmia / drug therapy*
  • Xerophthalmia / etiology
  • Xerophthalmia / metabolism


  • Ophthalmic Solutions
  • Polyphosphates
  • Purinergic P2Y Receptor Agonists
  • Uracil Nucleotides
  • diquafosol