Evaluation Of The Safety Of A Novel Preservative-Free Formulation Of Brimonidine Tartrate Ophthalmic Solution

Ocular redness, or conjunctival hyperemia, is a common ophthalmic sign associated with reduced quality of life. For redness without apparent underlying pathology, topical ophthalmic decongestants have been widely used.  Low-dose (0.025%) brimonidine tartrate ophthalmic solution was approved by the FDA in 2017 under the brand name LUMIFY and more recently in other European countries. For some, frequent exposure of the ocular surface to the preservative benzalkonium chloride can induce or exacerbate existing ocular irritation. Thus, a preservative-free formulation of brimonidine tartrate ophthalmic solution 0.025% (BTOS-PF) has been developed. Here we describe results from a study evaluating the efficacy and safety of BTOS-PF vs LUMIFY.

This was a multi-center, double-masked, randomized, active-controlled, parallel-group study in healthy adults (> 18 years of age) with ocular redness, conducted at 6 sites in the US. 

The study occurred over 5 weeks: Screening Visit for partipants (pts) (Day -28 to Day 1); Visit 1 (Baseline; Day 1); Visit 2 (Day 15 ± 2 days); Visit 3 (Day 29 + 2 days); and Visit 4 (Day 36 + 1 day). After the initial in-office dose at Visit 1, both agents were self-administered 4 times daily ~4 hours apart for a duration of 4 weeks. The primary efficacy endpoint was ocular redness score as evaluated by the Investigator prior to and at various timepoints after instillation at Visit 1. Safety variables included physical exam including vital signs, adverse events (AEs; reported, elicited, and observed), BCVA at distance, slit lamp biomicroscopy, IOP, dilated ophthalmoscopy, and ocular rebound. Clinical Study: NCT05360784.

380 pts were randomized 1:1 to receive BTOS-PF or LUMIFY, of which 378 received at least one dose of  LUMIFY and form the safety population. A total of 48 treatment-emergent AEs (TEAEs) were reported by 37 (19.7%) of 188 pts in the BTOS-PF group and 61 TEAEs reported by 39 (20.5%) of 190 pts in the LUMIFY group. There were 20 ocular TEAEs in 16 (8.5%) pts, and 28 non-ocular TEAEs in 23 (12.2%) pts in the BTOS-PF group; and 21 ocular TEAEs in 20 (10.5%) pts, and 40 non-ocular occurred in 22 (11.6%) pts in the LUMIFY group. Rates of ocular rebound were low and similar between treatment groups, 3 (1.8%) BTOS-PF group and 1 (0.6%) LUMIFY group. Tolerability, as measured by drop comfort assessment / questionnaire, was comparable between groups.

Overall, the safety profile of BTOS-PF was favorable and similar to that of LUMIFY.