lifitegrast ophthalmic (Rx)

>10%

Instillation site irritation (5-25%)

Dysgeusia (5-25%)

Reduced visual acuity (5-25%)

1-10%

Blurred vision (1-5%)

Conjunctival hyperemia (1-5%)

Eye irritation (1-5%)

Headache (1-5%)

Increased lacrimation (1-5%)

Eye discharge (1-5%)

Eye discomfort (1-5%)

Eye pruritus (1-5%)

Sinusitis (1-5%)

Postmarketing Reports

Serious hypersensitivity reactions, including anaphylactic reaction, bronchospasm, respiratory distress, pharyngeal edema, swollen tongue, urticaria, allergic conjunctivitis, dyspnea, angioedema, and allergic dermatitis; eye swelling and rash also reported

Contraindications

Hypersensitivity to drug or excipients

Cautions

Patients should not touch the tip of the single-use container to their eye or to any surface, in order to avoid eye injury or contamination of solution

Advise patients that contact lenses should be removed prior to administration; lenses can be reinserted 15 minutes after administration

Advise patients that the solution from one single-use container is to be used immediately after opening; can be used to dose both eyes

Single-use container, including any remaining contents, should be discarded immediately after administration

Pregnancy

There are no available data regarding use in pregnant women to inform any drug-associated risks

Animal data (IV administration)

• Lifitegrast administered daily by IV injection to rats, from premating through gestation day 17, caused an increase in mean preimplantation 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 recommended human ophthalmic dose (RHOD)
• In rabbits, an increased incidence of omphalocele was observed at the lowest dose tested, 3 mg/kg/day (400-fold the human plasma exposure at the RHOD, based on AUC), when administered by IV injection daily from gestation days 7 through 19

Lactation

There are no data on the presence of lifitegrast in human milk; systemic exposure to lifitegrast from ocular administration is low

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

The exact mechanism in dry eye disease is not known

Binds to the integrin lymphocyte function-associated antigen-1 (LFA-1), a cell surface protein bound on leukocytes, and blocks the interactions of LFA-1 with its cognate ligand intercellular adhesion molecule-1 (ICAM-1)

ICAM-1 may be overexpressed in corneal and conjunctival tissues in dry eye disease; LFA-1/ICAM-1 interaction can contribute to the formation of an immunological synapse resulting in T-cell activation and migration to target tissues

In vitro studies demonstrated that lifitegrast may inhibit T-cell adhesion to ICAM-1 in a human T-cell line and may inhibit secretion of inflammatory cytokines in human peripheral blood mononuclear cells

Absorption

Systemic absorption is low following ophthalmic administration

19% of patients studied had plasma lifitegrast trough concentration >0.5 ng/mL (the lower limit of assay quantitation)

Trough plasma concentrations that could be quantitated ranged from 0.55-3.74 ng/mL

Ophthalmic Administration

Drops are in single-use containers; discard the single-use container immediately after using in each eye

Remove contact lenses before instilling eye drops; may be reinserted 15 minutes following administration

Storage

Store at 20-25°C (68-77°F)

Store single-use containers in the original foil pouch