Dry Eye: An Overview of Investigational Treatments

Dry Eye: An Overview of Investigational Treatments

Dry eye disease is one of the most common conditions that eye care professionals encounter. Our treatment options are limited, but new medications are under development. These investigational dry eye therapies target different pathways in the disease process and include:

  • Diquafosol 3% from Merck is also known as Prolacria. This P2Y2 receptor agonist stimulates tear and mucin production to reduce the signs and symptoms of dry eye. It is well tolerated and has a good safety profile. In 2010, diquafosol received approval in Japan.
  • Rebamipide 2% from Otsuka Pharmaceuticals is a mucin secretagogue that serves as a mucosal protective drug that has been used in the treatment of gastric disorders and is approved in Japan for ulcers and gastritis. It has also been shown to improve dry eye symptoms and reduce corneal and conjunctival staining.
  • Lifitegrast 5% from Shire plc is a small molecule integrin antagonist that interferes with T-cell activation and cytokine release by inhibition of lymphocyte function-associated antigen 1 (LFA-1) and intercellular adhesion molecule 1 (ICAM-1). Lifitegrast reduces the ocular signs (corneal staining) and symptoms (discomfort and dryness) of dry eye.
  • Tofacitinib from Pfizer is an immunomodulator that is a Janus kinase 3 (JAK3) inhibitor that reduces HLA-DR expression in conjunctival cells with a resultant decrease in cytokine levels (e.g., MMP3, IL-1beta). It is approved for the treatment of rheumatoid arthritis and is now being studied as a topical dry eye therapy. Initial data indicate a trend for improving the signs and symptoms of dry eye, and the drug was well tolerated at both a 0.0003% and 0.005% concentration.
  • Anakinra 2.5% from Amgen is also known as Kineret and is a recombinant interleukin-1 receptor antagonist (IL-1Ra) that is used for the treatment of rheumatoid arthritis. Topical application of this medication reduces symptoms and corneal staining in patients with dry eye disease and is well tolerated.
  • EBI-005 from Eleven Biotherapeutics is a IL-1 signaling inhibitor (a chimera of IL-1beta and IL-1Ra) that improves dry eye signs and symptoms and is safe and well tolerated.
  • MIM-D3 from Mimetogen is a tyrosine kinase receptor agonist that increases mucin production. It demonstrates a protective effect on dry eye signs, reduces dry eye symptoms, and has a good safety profile.
  • R348 from Rigel Pharmaceuticals is a dual JAK and Syk (spleen tyrosine kinase) inhibitor that reduces inflammation and is well tolerated. Results from a preliminary study in patients with chronic dry eye are not yet available.

These and other treatments for dry eye disease are being evaluated around the world, so we may soon have more options at our disposal when treating patients who suffer from this common condition. Hopefully some of these novel therapies will be available in the near future.

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