Lifitegrast: Safety and Efficacy in Dry Eye Disease

Lifeset is an ophthalmic suspension, an immunomodulatory anti-inflammatory prescription medication for dry eye syndrome. It acts by inhibiting the binding of lymphocyte function-associated antigen-1 to intercellular adhesion molecule-1, thereby blocking T-cell activation and ocular surface infiltration. This reduces inflammation and alleviates symptoms including dryness, stinging, foreign body sensation, and corneal damage.

Safety of lifitegrast

Dry eye disease (DED) is a multifactorial chronic disorder of the ocular surface characterized by inflammation of the ocular surface and lacrimal glands, along with a reduction in tear quality or quantity. In 2016, Lifitegrast entered the market as the first approved drug for both the signs and symptoms of DED. It is a novel small molecule integrin antagonist that blocks the interaction between ICAM-1 and LFA-1, thus interrupting the T-cell mediated inflammatory cycle. Several clinical trials have demonstrated that Lifitegrast can significantly improve signs and symptoms of DED over a 12-week period and has shown favorable safety profiles during long-term use of up to one year, with the most common adverse reactions including decreased vision, pain at the site of administration, irritation at the site of administration, and reaction at the site of administration, mostly mild to moderate in nature. As one of the largest global databases for monitoring drug-related AEs, it provides a rich resource for studying medication safety. We utilized the FAERS database to identify adverse reactions reported during the post-marketing use of Lifitegrast and conducted a disproportionality analysis of these reactions. The findings from this study provide a scientific basis for clinical medication use, thereby enhancing patient drug safety.[1]

Through pharmacoepidemiological analysis utilizing the FAERS database, we identified ocular and systemic AE signals associated with Lifitegrast use in DED treatment, along with the temporal distribution characteristics of these AEs. Our study corroborated previously documented AEs such as eye irritation, eye pain, and eye swelling, while also uncovering novel ocular AEs including cataracts and glaucoma. Additionally, more AEs were reported among male patients and individuals aged 65 years or older.These findings underscore the importance of personalized monitoring for different genders and age groups in clinical practice and suggest that gender and age should be taken into account when formulating treatment plans. Although our research provides valuable evidence on the safety profile of Lifitegrast, it is important to acknowledge the inherent limitations of the FAERS database, particularly the potential impact on report quality and our analysis due to the majority of AE reports being submitted by patients. Future research should incorporate longer follow-up periods for monitoring AEs related to Lifitegrast. Prospective cohort studies and long-term clinical observations are warranted to confirm the phenomena and conclusions derived from this study.

Lifitegrast Ophthalmic Solution 5% as a Safe and Efficient Eyedrop

Dry eye disease (DED) is a multifactorial disease that causes ocular discomfort and visual impairment on a damaged ocular surface. Lifitegrast, a novel T-cell integrin antagonist, was approved in the United States in July 2016 as a 5% (50 mg/mL) ophthalmic solution for DED management. Currently, no meta-analysis and systemic review based on relevant studies have been conducted. This study aimed to evaluate the efficacy and safety of lifitegrast in patients with DED. We systematically searched Embase, Medline, PubMed, and Web of Science for randomized controlled trials (RCTs) and nonrandomized studies evaluating lifitegrast effects on symptomatic DED. Then, inferior corneal staining score, total corneal staining score (TCSS), nasal lissamine staining score (NLSS), total lissamine staining score, ocular discomfort score (ODS), eye discomfort score (visual analog scale (VAS) score), eye dryness score (EDS), ocular surface disease index score (OSDI-S), and tear break-up time (TBUT) were assessed. Clinical global impression and safety profiles were also evaluated.[2]

The studies were pooled in a random-effects model. We included five RCTs, one case–control study, and four longitudinal or retrospective studies, comprising 3197 participants. In the meta-analysis, lifitegrast was superior to the placebo because it improved TCSS, NLSS, TBUT, ODS, eye discomfort score, EDS, and OSDI-Sin DED. However, lifitegrast showed higher risks for ocular and non-ocular treatment-emergent adverse events (TEAEs) overall or at a mild or moderate level. Nonetheless, its incidence of adverse events slightly differed from that in the placebo, especially instillation site discomforts and dysgeusia, thereby considered safe and tolerable. Claims of withdrawal during follow-up caused by TEAEs were extremely rare. Lifitegrast improves DED, although dysgeusia, installation site pain, and irritation may be a concern for some. Overall, most of the adverse events are tolerable.

References

[1]Zhang C, Wang H, Chen X, Liu Y, Jiang P. Safety of lifitegrast: A real-world pharmacovigilance study based on FAERS. PLoS One. 2025 Apr 24;20(4):e0321307. doi: 10.1371/journal.pone.0321307. PMID: 40273175; PMCID: PMC12021224.

[2]Li JX, Tsai YY, Lai CT, Li YL, Wu YH, Chiang CC. Lifitegrast Ophthalmic Solution 5% Is a Safe and Efficient Eyedrop for Dry Eye Disease: A Systematic Review and Meta-Analysis. J Clin Med. 2022 Aug 26;11(17):5014. doi: 10.3390/jcm11175014. PMID: 36078948; PMCID: PMC9456613.

You may like