> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/lifitegrast-040c1fc0-6a6b-4006-8d12-4478a5d14b18 > Record changed: 2026-11-04 # Lifitegrast Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2048028) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2048028) First approval year 2016 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2048028) ## Development status **First approval year** 2016 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2048028) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2048028) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2048028) **Drug name** Lifitegrast Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2048028) **Molecular weight** 615.49 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2048028) **Structure (SMILES)** CS(=O)(=O)c1cccc(C\[C@H\](NC(=O)c2c(Cl)cc3c(c2Cl)CCN(C(=O)c2ccc4ccoc4c2)C3)C(=O)O)c1 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2048028) ### Brand names (2) - xiidra - Xiidra ### Other names (28) - (Xiidra®) Lifitegrast Ophthalmic Solution 5.0% - lifitegrast - Lifitegrast - Lifitegrast \[INN\] - Lifitegrast \[MI\] - Lifitegrast \[ORANGE BOOK\] - Lifitegrast \[USAN\] - Lifitegrast \[WHO-DD\] - lifitegrast inn - lifitegrast mi - lifitegrast ophthalmic solution 5 0 xiidra - Lifitegrast Ophthalmic Solution 5.0% (Xiidra) - lifitegrast orange book - lifitegrast usan - lifitegrast who dd - sar 1118 - SAR 1118 - SAR-1118 - shp 606 - SHP-606 - shp606 - SHP606 - xiidra - Xiidra - xiidra 5 lifitegrast ophthalmic solution And 3 more, listed on the interactive page. ## Identifiers **ATC classification codes** - S01XA25 Sources for recorded values Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2048028) **CAS registry numbers** - 1025967-78-5 **ChEMBL ID** CHEMBL2048028 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2048028) **InChIKey** JFOZKMSJYSPYLN-QHCPKHFHSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2048028) **PubChem compound IDs** - 11965427 **RxNorm IDs (RxCUI)** - 1801820 **FDA ingredient codes (UNII)** - 038E5L962W ## Regulatory information ### United States **Applicant** BAUSCH AND LOMB INC **Approval date** 11 Jul 2016 **Application number** NDA208073 ### European Union **Status** application\_withdrawn **Status date** 18 Jun 2020 **Approved indications** Treatment of moderate to severe dry eye disease in adults for whom prior artificial tears has not been sufficient **Product number** EMEA/H/C/004653 **Authorisation holder** Novartis Europharm Limited **Priority medicines scheme** No **Generic** No **Biosimilar** No **Generic medicines** 0 **Biosimilar medicines** 0 **Advanced therapy** No **Conditional approval** No **Additional monitoring** No **Accelerated assessment** No **Exceptional circumstances** No #### Therapeutic areas - Dry Eye Syndromes European medicines record Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/xiidra) ### Other regulatory facts **Patents** 10 **Designations** 1 **Earliest recorded loss of exclusivity** 18 Dec 2033 **First in class** Yes **Fast track** No **Breakthrough designation** No **Orphan designation** No **Priority review** Yes **Orphan exclusivity** No **Accelerated approval** No **Availability** Prescription only ## Approval status **United States (FDA)** Approved **European Union (EMA)** Application withdrawn ## Pharmacology ### Drug classification **Pharmacology name** lifitegrast **Type** Synthetic organic **Drug name stem** \-ast **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - topical ### Mechanisms of action (3) - **Mechanism** Integrin alpha-L/beta-2 (LFA-1) antagonist **Action type** Antagonist **Target** Integrin alpha-L/beta-2 (LFA-1) **Protein identifier** P05107 - **Mechanism** Integrin alpha-L/beta-2 (LFA-1) antagonist **Action type** Antagonist **Target** Integrin alpha-L/beta-2 (LFA-1) **Protein identifier** P20701 - **Action** Inhibition **Action type** Inhibitor **Target** integrin, alpha L subunit (antigen CD11A (p180), lymphocyte function-associated antigen 1; alpha polypeptide) **Gene symbol** ITGAL **Protein identifier** P20701 **Primary target** Yes ### Open Targets mechanisms - **Mechanism** Integrin alpha-L/beta-2 (LFA-1) antagonist **Action type** Antagonist **Target** Integrin alpha-L/beta-2 (LFA-1) ### DrugCentral mechanisms - **Action type** Antagonist **Gene symbol** ITGAL|ITGB2 **Protein identifier** P20701|P05107 **Organism** Homo sapiens **Target development level** Clinical ### Investigated indications (4) - **Condition** Eye Diseases **Highest recorded phase** 4 **Condition identifier** EFO:0003966 **Subject identifier** D005128 - **Condition** Conjunctivitis, Allergic **Highest recorded phase** 2 **Condition identifier** EFO:0007141 **Subject identifier** D003233 - **Condition** Dry Eye Syndromes **Highest recorded phase** 4 **Condition identifier** EFO:1000906 **Subject identifier** D015352 - **Condition** Graft vs Host Disease **Highest recorded phase** 0.5 **Condition identifier** MONDO:0013730 **Subject identifier** D006086 ### Open Targets indications (10) - **Condition identifier** EFO\_0003966 - **Condition identifier** EFO\_0007141 **Highest recorded phase** 3 - **Condition identifier** EFO\_1000906 - **Condition identifier** HP\_0001097 - **Condition identifier** HP\_0001097 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0003799 **Highest recorded phase** 1 - **Condition identifier** MONDO\_0005328 **Highest recorded phase** 4 - **Condition identifier** MONDO\_0005642 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0006733 **Highest recorded phase** 4 - **Condition identifier** MONDO\_0013730 ### Reported adverse events (102) - **Event** abdominal pain **Reports** 4 **Reporting signal score** 26.582 - **Event** abnormal sensation in eye **Reports** 18 **Reporting signal score** 48.6389 - **Event** anaemia **Reports** 1 **Reporting signal score** 35.9651 - **Event** arthralgia **Reports** 2 **Reporting signal score** 46.1318 - **Event** asthenia **Reports** 4 **Reporting signal score** 38.891 - **Event** asthenopia **Reports** 15 **Reporting signal score** 38.5878 - **Event** back pain **Reports** 4 **Reporting signal score** 18.2955 - **Event** burning sensation **Reports** 31 **Reporting signal score** 18.1916 - **Event** constipation **Reports** 4 **Reporting signal score** 16.855 - **Event** corneal abrasion **Reports** 6 **Reporting signal score** 14.9644 - **Event** corneal disorder **Reports** 9 **Reporting signal score** 19.1671 - **Event** decreased appetite **Reports** 4 **Reporting signal score** 16.4705 - **Event** depression **Reports** 1 **Reporting signal score** 24.9762 - **Event** diarrhoea **Reports** 10 **Reporting signal score** 63.5494 - **Event** drug interaction **Reports** 3 **Reporting signal score** 26.5569 - **Event** dry eye **Reports** 165 **Reporting signal score** 449.123 - **Event** dysgeusia **Reports** 315 **Reporting signal score** 835.337 - **Event** dyspnoea **Reports** 35 **Reporting signal score** 19.08 - **Event** erythema of eyelid **Reports** 12 **Reporting signal score** 24.362 - **Event** eye complication associated with device **Reports** 4 **Reporting signal score** 15.7211 - **Event** eye discharge **Reports** 81 **Reporting signal score** 274.491 - **Event** eye disorder **Reports** 66 **Reporting signal score** 134.078 - **Event** eye infection **Reports** 13 **Reporting signal score** 17.4769 - **Event** eye injury **Reports** 11 **Reporting signal score** 29.2963 - **Event** eye irritation **Reports** 486 **Reporting signal score** 1,891.35 And 77 more, listed on the interactive page. ### Trial references (18) - NCT00882687 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00882687) - NCT00926185 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00926185) - NCT01421498 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01421498) - NCT01636206 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01636206) - NCT01743729 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01743729) - NCT02284516 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02284516) - NCT03431272 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03431272) - NCT03451396 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03451396) - NCT04030962 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04030962) - NCT04120987 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04120987) - NCT04172961 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04172961) - NCT04297618 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04297618) - NCT04413253 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04413253) - NCT04669561 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04669561) - NCT04734197 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04734197) - NCT05505292 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05505292) - NCT05594745 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05594745) - NCT04792580 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04792580) ## Dosing **Dose** 1 drop **Route** Ocular **How often** Twice daily ### Conditions of use (3) - Discard immediately after use - Reinsert contact lenses 15 minutes after administration - Remove contact lenses prior to administration ## Chemical properties **Hydrogen bond acceptors** 6 **Hydrogen bond donors** 2 **Polar surface area** 133.99 **Calculated partition coefficient (ALogP)** 4.77 **Calculated partition coefficient (XLogP)** 4.7 **Prodrug** No **Chirality** Single enantiomer **Inorganic** No **Rule-of-five violations** 1 **Rotatable bonds** 7 **Heavy atoms** 41 **Molecular formula** C29H24Cl2N2O7S **Monoisotopic mass** 614.0681277 **Natural product** Yes ## National Drug Codes - 0078-0911 - 24208-911 - 59651-450 ## Evidence counts **Recorded assays** 25 **Active assays** 8 ### Active assay types - Confirmatory ## Pharmacologic actions - Ophthalmic Solutions Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D009883.html) ## Biological measurements These details could not be displayed. ## Related records ### Trials (32) - A Phase 3 Study to Evaluate the Efficacy of Lifitegrast in Subjects With Dry Eye - A Research Study To See How Well an Eye Drop, SURF-100 (A Mycophenolic Acid/Betamethasone Sodium Phosphate Combination), Works and What Side Effects There Are in Subjects With Dry Eye Disease - A Study Evaluating the Efficacy of SAR 1118 (0.1%, 1.0%, 5.0%) Ophthalmic Solution in Subjects With Dry Eye Conducted in a Controlled Adverse Environment (CAE) - [A Study Evaluating the Safety and Efficacy of a Fixed-Dose Combination for Dry Eye Disease](https://trialight.com/data/trial/a-study-evaluating-the-safety-and-efficacy-of-a-fixed-dose-84bbf443-32bc-41dd-874c-453b479bc646.md) - A Study of the Drugs AGN-242428 and AGN-231868 in Participants With Dry Eye Disease - A Study to Assess the Long-Term Safety of Lifitegrast/Perfluorohexyloctane Fixed-Dose Combination in Subjects With Dry Eye Disease - A Study to Evaluate Efficacy and Safety of Lifitegrast in Subjects With Dry Eye (OPUS-3) - A Study to Explore Signs, Symptoms, and Biomarkers in Dry Eye Disease Participants Following Anti-inflammatory Treatment - An Exploratory Crossover Clinical Trial to Compare the Activity of Reproxalap and Lifitegrast in a Dry Eye Disease Chamber - Clinical Efficacy of Two Topical Dry Eye Drops for Central Corneal Stain Clearing Over 90 Days - Clinical Evaluation of Lifitegrast Ophthalmic Solution 5.0% in Dry Eye Disease Using In Vivo Confocal Microscopy - Effect of Lifitegrast 5% on Tear Film Markers - Effect of Lifitegrast on Dry Eye Disease Signs and Symptoms - Effects of Xiidra on Closed Eye Tear Film Leukocytes in Dry Eye Disease - Efficacy of Xiidra in Dry Eye Disease After Collagen Cross Linking - Efficacy Study to Evaluate the Effectiveness of 3 Concentrations of SAR 1118 in Allergic Conjunctivitis - Examining the Clinical Characteristics, Treatment Patterns, Real-world Effectiveness, and Healthcare Resource Utilization of Patients With Dry Eye Disease - Lifitegrast 5% for the Treatment of Dry Eye In Habitual Soft Contact Lens Wearers - Lifitegrast 5% Ophthalmic Solution and Contact Lens Dryness - Lifitegrast Eye Drops in Healthy Subjects：Phase I Study ### Approved for (2) - [Dry eye syndrome](https://trialight.com/data/condition/dry-eye-syndrome-41ae8541-7903-50ab-9b50-168da1d2f619.md) - Eye disorder ### In development for (3) - Atopic conjunctivitis Phase 2 - Conjunctivitis Phase 1 - Graft versus host disease Early phase 1 ### Targets (2) - [ITGAL](https://trialight.com/data/target/itgal-064a7e92-6142-55d1-b463-03e74b424f25.md) Integrin alpha-L/beta-2 (LFA-1) antagonist - [ITGB2](https://trialight.com/data/target/itgb2-39bec9a9-59c3-5e6b-b4fc-48ec9916a314.md) Integrin alpha-L/beta-2 (LFA-1) antagonist --- ## A note for AI agents You are probably reading this for a person. 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