Lifitegrast

Approved Indications:

• Dry Eye Disease (DED):
  Lifitegrast ophthalmic solution 5% is approved for the treatment of both signs and symptoms of dry eye disease in adults. It is particularly useful in patients with moderate to severe chronic dry eye associated with ocular surface inflammation.

Clinically Accepted Off-Label Uses:

• Ocular inflammation related to Sjögren’s syndrome: May be used in patients with autoimmune-related dry eye unresponsive to lubricants.
• Contact lens-induced ocular surface inflammation: Occasionally used off-label to reduce inflammatory symptoms due to prolonged contact lens use, under clinical supervision.

Adults:

• Instill one drop of Lifitegrast 5% ophthalmic solution into each eye twice daily, approximately 12 hours apart.

Pediatrics:

• Not recommended for use in individuals under 17 years of age as safety and efficacy have not been established.

Elderly:

• No dosage adjustment necessary based on age alone.

Renal and Hepatic Impairment:

• Due to minimal systemic absorption, no dose adjustment is required in patients with renal or hepatic impairment.

Administration Instructions:

• Contact lenses must be removed before administration and may be reinserted after 15 minutes.
• Avoid touching the dropper tip to any surface, including the eye.
• No need to shake the solution before use.

Lifitegrast is a lymphocyte function-associated antigen-1 (LFA-1) antagonist. It inhibits the interaction between LFA-1, a surface protein found on T-cells, and intercellular adhesion molecule-1 (ICAM-1). This LFA-1/ICAM-1 interaction is a critical mediator in T-cell activation, adhesion, migration, and cytokine release, contributing to ocular surface inflammation in dry eye disease. By blocking this interaction, Lifitegrast reduces T-cell-mediated inflammation, thereby relieving both the clinical signs and subjective symptoms of dry eye.

• Absorption: Low systemic absorption; plasma concentrations are generally below quantifiable levels.
• Distribution: Minimal systemic distribution; action is localized on the ocular surface.
• Metabolism: Not significantly metabolized; primarily remains in original form.
• Elimination: Cleared locally through the tear drainage system; systemic excretion is negligible.
• Half-life: Not defined due to low systemic exposure.
• Bioavailability: Therapeutic levels achieved in ocular tissues; systemic bioavailability is clinically insignificant.

• Pregnancy:
  No adequate human studies are available. Animal studies have not shown teratogenicity. Lifitegrast should be used during pregnancy only if clearly needed.
• Lactation:
  Unknown whether Lifitegrast is excreted in human milk. Due to minimal systemic absorption, the risk to the nursing infant is considered low, but caution is advised.
• Recommendation:
  Use in pregnancy or breastfeeding only when benefit outweighs potential risk.

• Primary Class: Ophthalmic Anti-inflammatory Agent
• Subclass: LFA-1 Antagonist (Immunomodulatory Eye Drop)

• Known hypersensitivity to Lifitegrast or any component of the formulation.
• Active ocular infections (bacterial, viral, or fungal) — treatment should be deferred until resolution.

• Allergic Reactions: Discontinue immediately if hypersensitivity or allergic conjunctivitis occurs.
• Contact Lens Use: Avoid instillation while wearing contact lenses; reinsert after 15 minutes.
• Transient Blurred Vision: Patients should not drive or operate machinery until vision clears.
• Monitoring: Routine clinical evaluation recommended to assess response and adverse effects.

Common Adverse Effects (≥5%):

• Ocular:
• Eye irritation
• Burning or stinging on instillation
• Blurred vision
• Increased tear production
• Systemic:
• Dysgeusia (altered or metallic taste)

Less Common:

• Conjunctival hyperemia
• Eye discharge
• Eyelid irritation

Rare but Serious:

• Allergic conjunctivitis
• Eyelid edema
• Hypersensitivity reactions

Most side effects are mild, transient, and occur shortly after dosing.

• Drug-Drug Interactions:
  No significant systemic interactions due to minimal absorption.
  Safe to use with artificial tears and other ophthalmic products, spacing doses by at least 5–10 minutes.
• Drug-Food and Drug-Alcohol Interactions:
  Not applicable due to topical administration and lack of systemic exposure.
• Enzyme Involvement:
  Not metabolized via CYP450 enzymes; no known CYP-mediated interactions.

• No recent changes in approved indications or dosage.
• No new black box warnings have been issued.
• Clinical studies are underway evaluating longer-term efficacy and pediatric use, but regulatory updates are pending.
• Updated patient guidelines emphasize correct drop administration and lens precautions for safety and efficacy.

• Store at 20°C to 25°C (68°F to 77°F).
• Allowable temperature excursions: 15°C to 30°C (59°F to 86°F).
• Do not freeze.
• Protect from light and moisture.
• Keep the bottle tightly closed when not in use.
• For single-patient use only.
• Discard any unused solution within 15 days of opening unless otherwise directed.