Lifitegrast

XIIDRA

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Pronunciation: lif-i-TEG-rast (ZYE-dra)

Lifitegrast ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Lifitegrast ballicule

What it isLFA-1 antagonist blocking T-cell mediated inflammation; dry eye disease.

Why this oneIt targets the inflammation rather than only lubricating, and it works faster than cyclosporine drops.

What limits itAn intense unpleasant taste immediately after instillation is the usual reason for stopping.

Pearls

Remove contacts; reinsert 15 minutes after dosing.
Benefit modest; transient blurring and irritation common.

Lifitegrast molecular structure (skeletal formula) — Molecular structure: Lifitegrast

FDA-approved for

dry eye disease (2016)

Principal riskDysgeusia immediately after instillation

Classes and tags

Ophthalmic drugs

Clinical profile

Therapeutic safety burden0 / 4

Overdose danger0 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk0 / 4

Legacy pregnancy categoryNot assigned — PLLR-era drug

Defining liabilityLocal irritation, sensitization or administration-site injury; negligible systemic toxicity at usual use.

FDA label

Read the full label on DailyMed ↗

NO BOXED WARNINGS

FDA dosing	Population	Start	Target	Max
Dry eye disease	Adults	1 drop in each eye BID (~12h apart)	1 drop each eye BID	1 drop each eye BID

Renal Undefined

Hepatic Undefined

Instructions

Instill one drop into each eye twice daily (~12 hours apart) using a single-use container; discard immediately after using in each eye.
Remove contact lenses before administration; may reinsert 15 minutes afterward.

Available strengths

drops 5 %
sol 50 mg/mL

Cautions

Hypersensitivity reactions incl. anaphylaxis, bronchospasm, respiratory distress, angioedema (postmarketing)

Adverse reactions

Instillation-site irritation
Dysgeusia (altered taste)
Reduced/blurred visual acuity
Eye irritation/discomfort, conjunctival hyperemia, increased lacrimation, headache

Pregnancy No human data; low systemic exposure after ocular use; animal omphalocele at high IV doses of unclear relevance.

Lactation No data on presence in human milk; systemic exposure from ocular use is low.

Cost

Lifitegrast (XIIDRA)

Strength		#/mo	generic $/unit	CostPlus
5 %	drops	per unit		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Lifitegrast is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2023

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Self-check

What taste effect commonly causes lifitegrast discontinuation?
An intense unpleasant taste immediately after instillation.
How does lifitegrast’s onset compare with cyclosporine drops?
Faster.