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
Medically reviewed by Drugs.com. Last updated on Aug 18, 2020.
Uses for Lifitegrast
Dry Eye Disease
Lifitegrast Dosage and Administration
Remove contact lenses prior to administration; may reinsert lenses 15 minutes after administration.1
Sufficient amount of solution in each single-use container for administration of 1 dose into each eye.1 Preservative-free solution is for single use only; discard any unused portion immediately after administration.1 12
Dry Eye Disease
1 drop of a 5% solution in each eye twice daily, approximately 12 hours apart.1
No special population recommendations at this time.1
Cautions for Lifitegrast
Manufacturer states none known.1
No data available regarding use in pregnant women.1
Consider developmental and health benefits of breast-feeding along with mother's clinical need for the drug and any potential adverse effects of the drug on the infant.1
Safety and efficacy not established in pediatric patients <17 years of age.1
No overall differences in safety or efficacy relative to younger adults.1
Common Adverse Effects
Ocular effects: Instillation site irritation, reduced visual acuity, blurred vision, conjunctival hyperemia, irritation, increased lacrimation, discharge, discomfort, pruritus.1
Nonocular effects: Dysgeusia, headache, sinusitis.1
Interactions for Lifitegrast
Following topical administration of lifitegrast 5% solution to the eye twice daily for 180 and/or 360 days, 19% of patients had lifitegrast trough concentrations above the lower limit of quantitation (0.5 ng/mL).1 6
Not known whether distributed into milk after topical application to the eye.1
Interaction between LFA-1 and intercellular adhesion molecule-1 (ICAM-1) contributes to T-cell activation and migration to target tissues and secretion of inflammatory cytokines.1 7 8 Binding of lifitegrast to LFA-1 blocks interaction between LFA-1 and ICAM-1, thereby inhibiting T-cell adhesion to ICAM-1 and secretion of cytokines.1 7 8
Advice to Patients
Importance of learning and adhering to proper administration techniques to avoid eye injury or contamination of the ophthalmic solution.1
Importance of storing single-use containers in original foil pouch until ready to use.1
Importance of administering ophthalmic solution immediately after opening the single-use container and discarding any unused portion immediately after administration.1
If contact lenses are worn, importance of removing lenses prior to administration and delaying reinsertion of lenses for 15 minutes after administration.1
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1
Importance of informing patients of other important precautionary information.1 (See Cautions.)
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.
AHFS DI Essentials™. © Copyright 2021, Selected Revisions August 28, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
1. Shire US Inc. Xiidra (lifitegrast) ophthalmic solution prescribing information. Lexington, MA; 2016 Jul. http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ac09d19a-e321-4556-8a5c-66bd27cb6533
2. Holland EJ, Whitley WO, Sall K et al. Lifitegrast clinical efficacy for treatment of signs and symptoms of dry eye disease across three randomized controlled trials. Curr Med Res Opin. 2016; :1-7. http://www.ncbi.nlm.nih.gov/pubmed/27388660?dopt=AbstractPlus
3. Sheppard JD, Torkildsen GL, Lonsdale JD et al. Lifitegrast ophthalmic solution 5.0% for treatment of dry eye disease: results of the OPUS-1 phase 3 study. Ophthalmology. 2014; 121:475-83. http://www.ncbi.nlm.nih.gov/pubmed/24289915?dopt=AbstractPlus
4. Tauber J, Karpecki P, Latkany R et al. Lifitegrast Ophthalmic Solution 5.0% versus Placebo for Treatment of Dry Eye Disease: Results of the Randomized Phase III OPUS-2 Study. Ophthalmology. 2015; 122:2423-31. http://www.ncbi.nlm.nih.gov/pubmed/26365210?dopt=AbstractPlus
5. Donnenfeld ED, Karpecki PM, Majmudar PA et al. Safety of Lifitegrast Ophthalmic Solution 5.0% in Patients With Dry Eye Disease: A 1-Year, Multicenter, Randomized, Placebo-Controlled Study. Cornea. 2016; 35:741-8. http://www.ncbi.nlm.nih.gov/pubmed/27055211?dopt=AbstractPlus http://www.pubmedcentral.nih.gov/picrender.fcgi?tool=pmcentrez&artid=4859202&blobtype=pdf
6. Food and Drug Administration. Center for Drug Evaluation and Research: Application number 208073Orig1s000: Summary Review. From FDA website http://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208073Orig1s000SumR.pdf
7. Perez VL, Pflugfelder SC, Zhang S et al. Lifitegrast, a Novel Integrin Antagonist for Treatment of Dry Eye Disease. Ocul Surf. 2016; 14:207-15. http://www.ncbi.nlm.nih.gov/pubmed/26807723?dopt=AbstractPlus
8. Semba CP, Gadek TR. Development of lifitegrast: a novel T-cell inhibitor for the treatment of dry eye disease. Clin Ophthalmol. 2016; 10:1083-94. http://www.ncbi.nlm.nih.gov/pubmed/27354762?dopt=AbstractPlus http://www.pubmedcentral.nih.gov/picrender.fcgi?tool=pmcentrez&artid=4910612&blobtype=pdf
9. Holland EJ, Luchs J, Karpecki PM et al. Lifitegrast for the Treatment of Dry Eye Disease: Results of a Phase III, Randomized, Double-Masked, Placebo-Controlled Trial (OPUS-3). Ophthalmology. 2017; 124:53-60. http://www.ncbi.nlm.nih.gov/pubmed/28079022?dopt=AbstractPlus
10. Pflugfelder SC, Stern M, Zhang S et al. LFA-1/ICAM-1 Interaction as a Therapeutic Target in Dry Eye Disease. J Ocul Pharmacol Ther. 2017 Jan/Feb; 33:5-12.
11. Semba CP, Swearingen D, Smith VL et al. Safety and pharmacokinetics of a novel lymphocyte function-associated antigen-1 antagonist ophthalmic solution (SAR 1118) in healthy adults. J Ocul Pharmacol Ther. 2011; 27:99-104. http://www.ncbi.nlm.nih.gov/pubmed/20334535?dopt=AbstractPlus
12. Shire US Inc, Lexington, MA: Personal communication.
Frequently asked questions
- How long does it take for Xiidra to work?
- Can I use other eye drops with Xiidra?
- How much is Xiidra without insurance?
- How does Xiidra differ from OTC dry eye treatments?
More about lifitegrast ophthalmic
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