Lifitegrast

Lifitegrast binds to the integrin LFA-1, a cell surface protein found on leukocytes and blocks the interaction of LFA-1 with its cognate ligand intercellular adhesion molecule‑1 (ICAM-1). ICAM-1 may be overexpressed in corneal and conjunctival tissues in DED.

• Xiidra ® (lifitegrast ophthalmic solution) 5% is indicated for the treatment of the signs and symptoms of dry eye disease (DED). Xiidra (lifitegrast ophthalmic solution) 5% is a lymphocyte function-associated antigen-1 (LFA-1) antagonist indicated for the treatment of the signs and symptoms of dry eye disease (DED).

• Xiidra is contraindicated in patients with known hypersensitivity to lifitegrast or to any of the other ingredients in the formulation [see Adverse Reactions (6.2) ]. Hypersensitivity.contraindicated

Instill one drop of Xiidra twice daily (approximately 12 hours apart) into each eye using a single-use container. Discard the single‑use container immediately after using in each eye. Contact lenses should be removed prior to the administration of Xiidra and may be reinserted 15 minutes following administration. One drop twice daily in each eye (approximately 12 hours apart). ( 2 )

The following serious adverse reactions are described elsewhere in the labeling: Hypersensitivity [see Contraindications (4) ] The most common adverse reactions (incidence 5%-25%) following the use of Xiidra were instillation-site irritation, dysgeusia, and decreased visual acuity ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Bausch & Lomb Incorporated at 1-800-553-5340 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. In five clinical trials of DED conducted with lifitegrast ophthalmic solution, 1401 patients received at least one dose of lifitegrast (1287 of which received lifitegrast 5%). The majority of patients (84%) had less than or equal to 3 months of treatment exposure. One hundred-seventy patients were exposed to lifitegrast for approximately 12 months. The majority of the treated patients were female (77%). The most common adverse reactions reported in 5%-25% of patients were instillation-site irritation, dysgeusia, and reduced visual acuity. Other adverse reactions reported in 1%-5% of the patients were blurred vision, conjunctival hyperemia, eye irritation, headache, increased lacrimation, eye discharge, eye discomfort, eye pruritus, and sinusitis. 6.2 Postmarketing Experience The following adverse reactions have been identified during post-approval use of Xiidra.

8.1 Pregnancy Risk Summary There are no available data on Xiidra use in pregnant women to inform any drug-associated risks. Intravenous (IV) administration of lifitegrast to pregnant rats, from premating through gestation day 17, did not produce teratogenicity at clinically relevant systemic exposures. Intravenous administration of lifitegrast to pregnant rabbits during organogenesis produced an increased incidence of omphalocele at the lowest dose tested, 3 mg/kg/day (400-fold the human plasma exposure at the recommended human ophthalmic dose [RHOD], based on the area under the curve [AUC] level). Since human systemic exposure to lifitegrast following ocular administration of Xiidra at the RHOD is low, the applicability of animal findings to the risk of Xiidra use in humans during pregnancy is unclear [see Clinical Pharmacology (12.3) ] Data Animal Data Lifitegrast administered daily by IV injection to rats, from premating through gestation day 17, caused an increase in mean pre-implantation loss and an increased incidence of several minor skeletal anomalies at 30 mg/kg/day, representing 5,400-fold the human plasma exposure at the RHOD of Xiidra, based on AUC. No teratogenicity was observed in the rat at 10 mg/kg/day (460-fold the human plasma exposure at the RHOD, based on AUC).

Metabolism

In a subset of DED patients (n = 47) enrolled in a Phase 3 trial, the pre-dose (trough) plasma concentrations of lifitegrast were measured after 180 and 360 days of topical ocular dosing (one drop twice daily) with Xiidra (lifitegrast ophthalmic solution) 5%. A total of nine of the 47 patients (19%) had plasma lifitegrast trough concentrations above 0.5 ng/mL (the lower limit of assay quantitation).

• Jul 11, 2016NDANDA208073Bausch And Lomb Inc
• Nov 7, 2023ANDAANDA215063Eugia Pharma

1. 1Eye Irritation2,70617%
2. 2Vision Blurred2,61016%
3. 3Drug Ineffective1,5689.8%
4. 4Eye Pain1,4058.8%
5. 5Instillation Site Pain1,2838.0%
6. 6Dry Eye1,1467.2%
7. 7Dysgeusia1,0956.8%
8. 8Instillation Site Reaction1,0196.4%
9. 9Ocular Hyperaemia6794.2%
10. 10Lacrimation Increased6143.8%
11. 11Headache6093.8%
12. 12Visual Impairment5723.6%
13. 13Product Dose Omission Issue4432.8%
14. 14Eye Pruritus4292.7%
15. 15Eye Discharge3842.4%

The 10 most recently updated of 39 ClinicalTrials.gov registrations naming Lifitegrast as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study to Explore Signs, Symptoms, and Biomarkers in Dry Eye Disease Participants Following Anti-inflammatory Treatment
  Active not recruiting · Phase 4 · Interventional · 378 enrolled · Hoffmann-La Roche
  NCT07025811updated 2026-05-06
• Clinical Evaluation of Lifitegrast Ophthalmic Solution 5.0% in Dry Eye Disease Using In Vivo Confocal Microscopy
  Not yet recruiting · Phase 4 · Interventional · 30 enrolled · Toyos Clinic
  NCT07560735updated 2026-05-01
• This is a Single Center, Open-label Prospective Study to Evaluate the Effect of Xiidra® (Lifitegrast Ophthalmic Solution 5.0%) on Tear Film Biomarkers in Dry Eye
  Not yet recruiting · Phase 4 · Interventional · 36 enrolled · Pittsburgh Research Institute
  NCT07490535updated 2026-03-24
• Treatment of Ocular Discomfort in Glaucoma Patients Using Multiple Topical Medications
  Recruiting · Observational · 75 enrolled · University of California, Los Angeles
  NCT04354545updated 2026-03-13
• A Study Evaluating the Safety and Efficacy of a Fixed-Dose Combination for Dry Eye Disease
  Recruiting · Phase 2 · Interventional · 423 enrolled · Bausch & Lomb Incorporated
  NCT07128628updated 2026-03-13
• A Study to Assess the Long-Term Safety of Lifitegrast/Perfluorohexyloctane Fixed-Dose Combination in Subjects With Dry Eye Disease
  Withdrawn · Phase 3 · Interventional · 0 enrolled · Bausch & Lomb Incorporated
  NCT07111013updated 2025-12-10
• Switching From Xiidra to TRYPTYR
  Not yet recruiting · Phase 4 · Interventional · 100 enrolled · Southern College of Optometry
  NCT07267481updated 2025-12-05
• Lifitegrast Eye Drops in Healthy Subjects：Phase I Study
  Completed · Phase 1 · Interventional · 24 enrolled · Qilu Pharmaceutical Co., Ltd.
  NCT07040826updated 2025-06-27
• A Study of the Drugs AGN-242428 and AGN-231868 in Participants With Dry Eye Disease
  Completed · Phase 1 · Phase 2 · Interventional · 292 enrolled · AbbVie
  NCT04030962updated 2025-05-20
• A Research Study To See How Well an Eye Drop, SURF-100 (A Mycophenolic Acid/Betamethasone Sodium Phosphate Combination), Works and What Side Effects There Are in Subjects With Dry Eye Disease
  Completed · Phase 2 · Interventional · 349 enrolled · Surface Ophthalmics, Inc.
  NCT04734197updated 2025-05-11

Frequently asked questions

How does Lifitegrast work?

Lifitegrast binds to the integrin LFA-1, a cell surface protein found on leukocytes and blocks the interaction of LFA-1 with its cognate ligand intercellular adhesion molecule‑1 (ICAM-1). ICAM-1 may be overexpressed in corneal and conjunctival tissues in DED.

What is Lifitegrast used for?

According to FDA labeling, Lifitegrast carries indications including: Xiidra ® (lifitegrast ophthalmic solution) 5% is indicated for the treatment of the signs and symptoms of dry eye disease (DED). Xiidra (lifitegrast ophthalmic solution) 5% is a lymphocyte function-associated antigen-1 (LFA-1) antagonist indicated for the treatment of the signs and symptoms of dry eye disease (DED).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Lifitegrast?

Lifitegrast is classified as Other ophthalmologicals, Lymphocyte Function-Associated Antigen-1 Antagonist, Lymphocyte Function-Associated Antigen-1 Antagonists, Decreased Immunologic Activity, Decreased T Lymphocyte Activation.

What are the brand names for Lifitegrast?

Lifitegrast is marketed under brand names including Xiidra.

What are the contraindications for Lifitegrast?

Lifitegrast labeling lists contraindications including: Xiidra is contraindicated in patients with known hypersensitivity to lifitegrast or to any of the other ingredients in the formulation [see Adverse Reactions (6.2) ]. Hypersensitivity.. Always consult the full prescribing information and a clinician.