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Class: Anti-inflammatory Agents, Miscellaneous
Chemical Name: (2S)-2-[[2-(1-benzofuran-6-carbonyl)-5,7-dichloro-3,4-dihydro-1H-isoquinoline-6-carbonyl]amino]-3-(3-methylsulfonylphenyl)propanoic acid
Molecular Formula: C29H24Cl2N2O7S
CAS Number: 1025967-78-5
Brands: Xiidra


Lifitegrast, a lymphocyte function-associated antigen-1 (LFA-1) antagonist, is an anti-inflammatory agent.

Uses for Lifitegrast

Lifitegrast has the following uses:

Lifitegrast ophthalmic solution 5% is a lymphocyte function-associated antigen-1 (LFA-1) antagonist indicated for the treatment of the signs and symptoms of dry eye disease (DED).1

Lifitegrast Dosage and Administration


Lifitegrast is available in the following dosage form(s) and strength(s):

Ophthalmic solution containing lifitegrast 5% (50 mg/mL).1


It is essential that the manufacturer’s labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:

One drop twice daily in each eye (approximately 12 hours apart).1

Cautions for Lifitegrast




Information not available.

Please see product labeling for general warning and precaution information.

Specific Populations


There are no available data on lifitegrast use in pregnant women to inform any drug associated risks. Intravenous (IV) administration of lifitegrast to pregnant rats, from pre-mating through gestation day 17, did not produce teratogenicity at clinically relevant systemic exposures. Intravenous administration of lifitegrast to pregnant rabbits during organogenesis produced an increased incidence of omphalocele at the lowest dose tested, 3 mg/kg/day (400-fold the human plasma exposure at the recommended human ophthalmic dose [RHOD], based on the area under the curve [AUC] level). Since human systemic exposure to lifitegrast following ocular administration of lifitegrast at the RHOD is low, the applicability of animal findings to the risk of lifitegrast use in humans during pregnancy is unclear. 1

Lifitegrast administered daily by intravenous (IV) injection to rats, from pre-mating 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 RHOD of lifitegrast, based on AUC. No teratogenicity was observed in the rat at 10 mg/kg/day (460-fold the human plasma exposure at the RHOD, based on AUC). In the rabbit, 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. A fetal No Observed Adverse Effect Level (NOAEL) was not identified in the rabbit.1


There are no data on the presence of lifitegrast in human milk, the effects on the breastfed infant, or the effects on milk production. However, systemic exposure to lifitegrast from ocular administration is low. The developmental and health benefits of breastfeeding should be considered, along with the mother’s clinical need for lifitegrast and any potential adverse effects on the breastfed child from lifitegrast.1

Pediatric Use

Safety and efficacy in pediatric patients below the age of 17 years have not been established.1

Geriatric Use

No overall differences in safety or effectiveness have been observed between elderly and younger adult patients.1

Common Adverse Effects

The most common adverse reactions (incidence 5-25%) following the use of lifitegrast were instillation site irritation, dysgeusia and decreased visual acuity.1

Drug Interactions

Specific Drugs

It is essential that the manufacturer’s labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights:

Please see product labeling for drug interaction information.


Mechanism Of Action

Lifitegrast binds to the integrin lymphocyte function-associated antigen-1 (LFA-1), a cell surface protein found on leukocytes, and blocks the interaction 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 vitrostudies 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. The exact mechanism of action of lifitegrast in dry eye disease is not known.1

Advice to Patients

Advise patients to read the FDA-approved patient labeling.1

Handling the Single-use Container

Advise patients not to touch the tip of the single-use container to their eye or to any surface, in order to avoid eye injury or contamination of the solution.1

Use with Contact Lenses

Advise patients that contact lenses should be removed prior to administration of lifitegrast and can be reinserted 15 minutes after administration.1


Advise patients that the solution from one single-use container is to be used immediately after opening. It can be used to dose both eyes. The single-use container, including any remaining contents should be discarded immediately after administration.1

Storage Information

Instruct patients to store single-use containers in the original foil pouch until ready to use.1

Additional Information

AHFS First Release. For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.



Dosage Forms


Brand Names



Solution/ Drops

5% (50 mg/mL)


Shire US Manufacturing Inc.

AHFS Drug Information. © Copyright 2017, Selected Revisions September 16, 2016. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.


1. Shire US Manufacturing Inc.. Xiidra (Lifitegrast) OPHTHALMIC prescribing information. 2016 Jul.