Lifitegrast
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2016
- First approval year
- 2016
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Lifitegrast
- Molecular weight
- 615.49
- Structure (SMILES)
- CS(=O)(=O)c1cccc(C[C@H](NC(=O)c2c(Cl)cc3c(c2Cl)CCN(C(=O)c2ccc4ccoc4c2)C3)C(=O)O)c1
- xiidra
- Xiidra
- (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.
- ATC classification codes
- S01XA25
Sources for recorded values
- CAS registry numbers
- 1025967-78-5
- ChEMBL ID
- CHEMBL2048028
- InChIKey
- JFOZKMSJYSPYLN-QHCPKHFHSA-N
- PubChem compound IDs
- 11965427
- RxNorm IDs (RxCUI)
- 1801820
- FDA ingredient codes (UNII)
- 038E5L962W
- Applicant
- BAUSCH AND LOMB INC
- Approval date
- 11 Jul 2016
- Application number
- NDA208073
- 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
- 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
- United States (FDA)
- Approved
- European Union (EMA)
- Application withdrawn
- Pharmacology name
- lifitegrast
- Type
- Synthetic organic
- Drug name stem
- -ast
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- topical
- 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
- 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
- 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
- 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.
- NCT00882687
- NCT00926185
- NCT01421498
- NCT01636206
- NCT01743729
- NCT02284516
- NCT03431272
- NCT03451396
- NCT04030962
- NCT04120987
- NCT04172961
- NCT04297618
- NCT04413253
- NCT04669561
- NCT04734197
- NCT05505292
- NCT05594745
- NCT04792580
- Dose
- 1 drop
- Route
- Ocular
- How often
- Twice daily
- Discard immediately after use
- Reinsert contact lenses 15 minutes after administration
- Remove contact lenses prior to administration
- 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
- 0078-0911
- 24208-911
- 59651-450
- Recorded assays
- 25
- Active assays
- 8
Active assay types
- Confirmatory
- Ophthalmic Solutions
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
- 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
- Eye disorder
In development for (3)
- Atopic conjunctivitis Phase 2
- Conjunctivitis Phase 1
- Graft versus host disease Early phase 1