Efficacy of epinastine hydrochloride ophthalmic solution in allergic conjunctivitis by conjunctival cedar pollen allergen challenge

Ann Allergy Asthma Immunol. 2014 Oct;113(4):476-81. doi: 10.1016/j.anai.2014.07.007. Epub 2014 Aug 20.


Background: Epinastine hydrochloride is a selective histamine H1 receptor antagonist that also inhibits IgE receptor-mediated histamine release from mast cells.

Objective: To show the superiority of epinastine 0.05% ophthalmic solution (epinastine) to placebo ophthalmic solution (placebo) and noninferiority to olopatadine 0.1% ophthalmic solution (olopatadine) for cedar pollen antigen-induced ocular itching and conjunctival hyperemia.

Methods: The study was conducted in ophthalmologically asymptomatic adult volunteers with seasonal allergic conjunctivitis using a conjunctival allergen challenge test. Subjects were randomized into 3 groups (n = 87) to evaluate superiority to placebo (visits 4 to 6) and 2 groups (n = 86) to evaluate noninferiority to olopatadine (visit 7). At each visit, a single administration of the study medication was instilled at 15 minutes (visit 4), 4 hours (visit 5), 8 hours (visit 6), and 4 hours (visit 7) before the conjunctival allergen challenge test. Ocular itching and conjunctival hyperemia of allergic conjunctivitis were assessed after the conjunctival allergen challenge test.

Results: For the primary end point, epinastine showed superiority to placebo for the inhibition of ocular itching and conjunctival hyperemia induced at 4 hours after the dose (equivalent to 4-times-daily dosing). For the secondary end points, epinastine significantly inhibited itching and conjunctival hyperemia induced at 15 minutes and 8 hours after the dose (equivalent to 2-times-daily dosing) compared with placebo. In addition, epinastine demonstrated noninferiority to olopatadine for ocular itching and conjunctival hyperemia. No adverse drug reactions or serious adverse events were reported throughout the study, indicating that epinastine has a good safety profile.

Conclusion: Epinastine is effective and safe for the treatment of allergic conjunctivitis.

Trial registration: Clinicaltrials.gov identifier NCT01363700.

Publication types

  • Clinical Trial, Phase III
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Allergens / immunology
  • Anti-Allergic Agents / adverse effects
  • Anti-Allergic Agents / therapeutic use*
  • Cedrus / immunology
  • Conjunctiva / immunology
  • Conjunctivitis, Allergic / drug therapy*
  • Dibenzazepines / adverse effects
  • Dibenzazepines / therapeutic use*
  • Dibenzoxepins / therapeutic use
  • Female
  • Histamine H1 Antagonists / adverse effects
  • Histamine H1 Antagonists / therapeutic use*
  • Humans
  • Hyperemia / drug therapy
  • Hyperemia / prevention & control
  • Imidazoles / adverse effects
  • Imidazoles / therapeutic use*
  • Male
  • Middle Aged
  • Olopatadine Hydrochloride
  • Ophthalmic Solutions / adverse effects
  • Ophthalmic Solutions / therapeutic use*
  • Platelet Aggregation Inhibitors / adverse effects
  • Platelet Aggregation Inhibitors / therapeutic use
  • Pollen / immunology
  • Rhinitis, Allergic, Seasonal / drug therapy
  • Young Adult


  • Allergens
  • Anti-Allergic Agents
  • Dibenzazepines
  • Dibenzoxepins
  • Histamine H1 Antagonists
  • Imidazoles
  • Ophthalmic Solutions
  • Platelet Aggregation Inhibitors
  • Olopatadine Hydrochloride
  • epinastine

Associated data

  • ClinicalTrials.gov/NCT01363700