1 drop in each eye BID, approximately 12 hours apart, from a single-use container
Eye dryness score separates from placebo by day 14 and holds through day 84.
OFF-LABELNot in the FDA label for this product
Ocular chronic graft-versus-host disease
1 drop in each eye BID, the labeled dry eye regimen, dosed BID for 4 weeks in the randomized trial
RCT · n=16 · underpowered
Single-center randomized double-masked vehicle-controlled trial: 32 enrolled, 16 analyzed (10 treated, 6 vehicle). SANDE symptom score fell 26.0 mm versus a 3.2 mm rise on vehicle (p=0.049) and median unanesthetized Schirmer rose 0.5 mm versus a 3 mm fall (p=0.014) at 4 weeks, while OSDI, corneal fluorescein staining, tear breakup time, and lid margin measures did not separate and temporal lissamine green staining was the only stain measure that did (p=0.048); the authors describe the trial as underpowered after a 50% dropout. A retrospective single-institution cohort of 18 allogeneic transplant recipients reported improved NIH ocular GVHD severity scores in 8 (44%). A single case report describes bacterial keratitis and corneal perforation requiring evisceration in a chronic GVHD patient on this drug, which its authors judged strongly associated with the drug by drug accountability criteria; the product owner and the authors then published replies to each other.
Known hypersensitivity to lifitegrast or to any other ingredient in the formulation.
Available Forms
5% (50 mg/mL) solution, 0.2 mL single-use containers, carton of 60 (12 foil pouches of 5)
Mechanism of Action
Lymphocyte function-associated antigen-1 (LFA-1) antagonist: binds the integrin LFA-1 on leukocytes and blocks its interaction with ICAM-1, which may be overexpressed in corneal and conjunctival tissue in dry eye disease, interrupting the immunological synapse that drives T-cell activation and migration into target tissue. In vitro it inhibits T-cell adhesion to ICAM-1 and inhibits inflammatory cytokine secretion from peripheral blood mononuclear cells; the label states the exact mechanism in dry eye disease is not known.
Warnings & Precautions
Hypersensitivity: Rare serious postmarketing reactions including anaphylactic reaction, bronchospasm, respiratory distress, pharyngeal edema, and angioedema; the product is contraindicated after hypersensitivity to any component.
Contact lens wear: Remove lenses before instillation and reinsert 15 minutes afterward.
Container tip contamination: Contact between the single-use container tip and the eye or any surface risks eye injury and contamination of the solution.
Common Side Effects
Ocular, 5% to 25%: Instillation-site irritation, reduced visual acuity.
Hypersensitivity, postmarketing: Rare serious reactions including anaphylaxis, bronchospasm, respiratory distress, pharyngeal edema, swollen tongue, angioedema, urticaria, allergic conjunctivitis, dyspnea, and allergic dermatitis; eye swelling and rash also reported.
Tolerability, pooled trials: Dysgeusia 14.5% versus 0.3% on placebo, instillation-site irritation 15.2% versus 2.8%, instillation-site reaction 12.3% versus 2.3%, instillation-site pain 9.8% versus 2.1%, discontinuation for adverse events 7.0% versus 2.6% (1287 treated, 1177 placebo).
Pregnancy & Lactation
Pregnancy: No human data. IV dosing in pregnant rats produced no teratogenicity at clinically relevant systemic exposures, with increased pre-implantation loss and several minor skeletal anomalies only at 5,400 times human plasma exposure at the recommended ophthalmic dose; in rabbits, omphalocele incidence rose at the lowest dose tested, 3 mg/kg/day (400 times that exposure by AUC), and no fetal NOAEL was identified. Systemic exposure after ocular dosing is low, so the applicability of the animal findings is unclear.
Lactation: No data on presence in human milk, effects on the breastfed infant, or milk production; systemic exposure after ocular administration is low.
Available Forms
Mechanism of Action
Pregnancy & Lactation
Pediatric Use