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Lymphocyte Function-Associated Antigen-1 (LFA-1) Antagonists

Ophthalmic Administration

Each dose is packaged in a single-use container. Prior to use, containers should be stored in the original foil pouch.
Wash hands before administering the drug.
Remove contact lenses. Contact lenses my be reinserted 15 minutes after drug administration.
Remove 1 single-use container from the foil pouch. Hold the container upright, and verify solution is at the bottom of the container. Open the container by twisting off the tab. Use caution to avoid touching the tip of the container to any surface.
Tilt head backwards or lie down.
Place the container close to the eye, without the eye touching the container tip. Gently squeeze to instill 1 drop onto lower eyelid and eye. Repeat process for the second eye. There is enough solution in each single-use container for both eyes.
Discard the single-use container immediately after use.

Adverse Reactions

visual impairment / Early / 5.0-25.0
angioedema / Rapid / Incidence not known
bronchospasm / Rapid / Incidence not known
anaphylactoid reactions / Rapid / Incidence not known


conjunctival hyperemia / Early / 1.0-5.0
blurred vision / Early / 1.0-5.0
conjunctivitis / Delayed / Incidence not known
ocular inflammation / Early / Incidence not known
dyspnea / Early / Incidence not known


dysgeusia / Early / 5.0-25.0
headache / Early / 1.0-5.0
ocular irritation / Rapid / 1.0-5.0
sinusitis / Delayed / 1.0-5.0
ocular discharge / Delayed / 1.0-5.0
lacrimation / Early / 1.0-5.0
ocular pruritus / Rapid / 1.0-5.0
urticaria / Rapid / Incidence not known
rash / Early / Incidence not known

Common Brand Names


Dea Class



Topical ophthalmic agent
Lymphocycte function-association antigen-1 antagonist
Used for dry eye disease

Dosage And Indications
For the treatment of dry eye disease. Ophthalmic dosage (5% ophthalmic solution) Adults

1 drop in each eye twice daily, approximately 12 hours apart.

Adolescents 17 years

1 drop in each eye twice daily, approximately 12 hours apart.

Dosing Considerations
Hepatic Impairment

Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

Renal Impairment

Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

Drug Interactions

There are no drug interactions associated with Lifitegrast products.

How Supplied

Lifitegrast/XIIDRA Ophthalmic Sol: 5%

Maximum Dosage

2 drops/day in each eye.


2 drops/day in each eye.


17 years: 2 drops/day in each eye.
< 17 years: Safety and efficacy have not been established.


Safety and efficacy have not been established.


Safety and efficacy have not been established.


Safety and efficacy have not been established.

Mechanism Of Action

The exact mechanism of action of lifitegrast in the treatment of dry eye disease is unknown. It is theorized that the mechanism involves blocking the interaction between lymphocyte function-associated antigen-1 (LFA-1) and its ligand intracellular adhesion molecule-1 (ICAM-1). ICAM-1, which may be overexpressed in corneal and conjunctival tissues of patients with dry eye disease, binds to the LFA-1, a surface protein found on lymphocytes. This interaction contributes to the formation of an immunological synapse that results in T-cell activation and migration to target tissues. In vitro data suggests that by blocking this interaction, lifitegrast inhibits T-cell adhesion to ICAM-1 and may inhibit secretion of inflammatory cytokines in human peripheral blood mononuclear cells.


Lifitegrast is administered topically to the eyes. Pharmacokinetic data are limited.
Affected cytochrome P450 isoenzymes: None

Other Route(s)

Ophthalmic Route
During one pharmacokinetic study, lifitegrast tough concentrations were measured in 47 patients with dry eye disease who were administered 1 drop twice daily via the ophthalmic route for 180 and 360 days. Measurable concentrations (i.e., greater than 0.5 ng/mL) were obtained in 9 of the 47 patients (19%), and ranged from 0.55 ng/mL to 3.74 ng/mL.

Pregnancy And Lactation

Data are not available regarding use of lifitegrast during human pregnancy. In animal studies, rats experienced an increase in mean preimplantation loss and an increased incidence of skeletal abnormalities when administered daily intravenous doses that produced exposures equivalent to 5,400-fold the human plasma exposure at the recommended human ophthalmic dose (RHOD). In addition, rabbits experienced an increased incidence of omphalocele when administered intravenous doses producing exposures 400-fold the human exposure at RHOD. However, since human exposure following ophthalmic administration is low, the applicability of animal findings to human fetal risk is unknown. Before administering lifitegrast during pregnancy, consider the benefits of treatment verse the potential risk to the infant.

No data are available regarding excretion of lifitegrast into human breast milk. However, because systemic drug concentrations are low following ophthalmic administration, significant amounts of the drug are not be expected to be excreted in breast milk. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, healthcare providers are encouraged to report the adverse effect to the FDA.