lifitegrast 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
integrin antagonists 5174 1025967-78-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lifitegrast
  • SAR 1118-023
  • SAR 1118
  • SAR-1118
  • xiidra
a lymphocyte function-associated antigen-1 ( LFA-1) antagonist, blocks the interaction of LFA-1 with its cognate ligand intercellular adhesion molecule-1 (ICAM-1), LFA-1/ICAM-1 interaction can contribute to the formation of an immunological synapse resulting in T-cell activation and migration to target tissues
  • Molecular weight: 615.48
  • Formula: C29H24Cl2N2O7S
  • CLOGP: 2.28
  • LIPINSKI: 1
  • HAC: 9
  • HDO: 2
  • TPSA: 133.99
  • ALOGS: -5.03
  • ROTB: 7

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
July 11, 2016 FDA SHIRE DEV LLC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Instillation site pain 2900.96 35.61 400 6603 463 56284601
Instillation site reaction 2283.19 35.61 300 6703 149 56284915
Eye irritation 1723.02 35.61 411 6592 18617 56266447
Vision blurred 1331.20 35.61 465 6538 82478 56202586
Dysgeusia 772.47 35.61 260 6743 40655 56244409
Instillation site irritation 593.54 35.61 78 6925 37 56285027
Instillation site pruritus 555.02 35.61 71 6932 14 56285050
Instillation site erythema 513.11 35.61 67 6936 27 56285037
Eye pain 480.29 35.61 170 6833 30677 56254387
Instillation site lacrimation 428.86 35.61 54 6949 3 56285061
Dry eye 423.20 35.61 161 6842 35555 56249509
Ocular hyperaemia 329.94 35.61 118 6885 21861 56263203
Lacrimation increased 280.95 35.61 100 6903 18248 56266816
Eye discharge 264.90 35.61 72 6931 5381 56279683
Instillation site discharge 258.31 35.61 33 6970 6 56285058
Instillation site swelling 215.84 35.61 27 6976 0 56285064
Product container issue 206.65 35.61 46 6957 1488 56283576
Eye pruritus 193.33 35.61 71 6932 14135 56270929
Product quality issue 171.13 35.61 82 6921 31654 56253410
Instillation site discomfort 167.87 35.61 21 6982 0 56285064
Ocular discomfort 147.54 35.61 42 6961 3713 56281351
Visual impairment 143.31 35.61 98 6905 74104 56210960
Product use complaint 141.53 35.61 36 6967 2073 56282991
Eye disorder 116.78 35.61 55 6948 20397 56264667
Instillation site dryness 92.46 35.61 12 6991 4 56285060
Eyelid margin crusting 89.82 35.61 21 6982 847 56284217
Instillation site inflammation 87.92 35.61 11 6992 0 56285064
Product packaging quantity issue 87.78 35.61 22 6981 1192 56283872
Foreign body sensation in eyes 86.83 35.61 24 6979 1903 56283161
Eye swelling 82.25 35.61 44 6959 21332 56263732
Instillation site foreign body sensation 77.31 35.61 10 6993 3 56285061
Taste disorder 74.12 35.61 32 6971 9683 56275381
Instillation site burn 71.94 35.61 9 6994 0 56285064
Inappropriate schedule of product administration 70.47 35.61 68 6935 83319 56201745
Superficial injury of eye 68.33 35.61 13 6990 188 56284876
Instillation site hypersensitivity 55.95 35.61 7 6996 0 56285064
Product taste abnormal 51.79 35.61 16 6987 1872 56283192
Product dose omission issue 48.11 35.61 89 6914 204664 56080400
Instillation site paraesthesia 47.96 35.61 6 6997 0 56285064
Swelling of eyelid 47.47 35.61 16 6987 2469 56282595
Madarosis 45.87 35.61 16 6987 2737 56282327
Asthenopia 37.96 35.61 13 6990 2104 56282960
Product dispensing issue 35.96 35.61 7 6996 115 56284949

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Instillation site reaction 604.20 100.89 67 1068 19 31696190
Vision blurred 547.63 100.89 149 986 41766 31654443
Instillation site pain 506.86 100.89 58 1077 40 31696169
Eye irritation 467.98 100.89 93 1042 6425 31689784
Lacrimation increased 136.34 100.89 35 1100 7447 31688762
Instillation site lacrimation 129.41 100.89 14 1121 0 31696209
Dry eye 105.30 100.89 29 1106 8043 31688166
Eye pain 101.72 100.89 31 1104 12273 31683936

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Instillation site pain 2348.68 45.22 292 3423 394 70924335
Instillation site reaction 1836.05 45.22 218 3497 129 70924600
Vision blurred 827.13 45.22 271 3444 94713 70830016
Eye irritation 550.19 45.22 137 3578 17651 70907078
Instillation site irritation 430.85 45.22 50 3665 14 70924715
Instillation site erythema 422.01 45.22 49 3666 14 70924715
Dysgeusia 415.58 45.22 138 3577 49364 70875365
Instillation site pruritus 364.08 45.22 42 3673 9 70924720
Instillation site lacrimation 304.63 45.22 35 3680 6 70924723
Eye pain 189.21 45.22 70 3645 34032 70890697
Instillation site swelling 186.06 45.22 21 3694 0 70924729
Ocular hyperaemia 179.86 45.22 62 3653 24577 70900152
Product quality issue 159.50 45.22 60 3655 30501 70894228
Instillation site discomfort 159.47 45.22 18 3697 0 70924729
Instillation site discharge 159.47 45.22 18 3697 0 70924729
Eye discharge 148.37 45.22 38 3677 5409 70919320
Lacrimation increased 141.03 45.22 49 3666 19850 70904879
Dry eye 111.24 45.22 47 3668 32235 70892494
Product container issue 110.10 45.22 22 3693 1020 70923709
Eye pruritus 88.28 45.22 32 3683 14615 70910114
Instillation site burn 79.73 45.22 9 3706 0 70924729
Visual impairment 73.36 45.22 48 3667 80202 70844527
Instillation site inflammation 70.87 45.22 8 3707 0 70924729
Product dose omission issue 68.96 45.22 70 3645 217398 70707331
Instillation site foreign body sensation 62.01 45.22 7 3708 0 70924729
Eye swelling 54.50 45.22 26 3689 23588 70901141
Inappropriate schedule of product administration 52.27 45.22 44 3671 107511 70817218
Foreign body sensation in eyes 50.86 45.22 13 3702 1829 70922900
Instillation site dryness 50.72 45.22 6 3709 3 70924726
Product use complaint 50.27 45.22 13 3702 1915 70922814
Eye disorder 45.28 45.22 22 3693 20763 70903966

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC S01XA25 SENSORY ORGANS
OPHTHALMOLOGICALS
OTHER OPHTHALMOLOGICALS
Other ophthalmologicals
MeSH PA D009883 Ophthalmic Solutions
MeSH PA D019999 Pharmaceutical Solutions
FDA MoA N0000192700 Lymphocyte Function-Associated Antigen-1 Antagonists
FDA EPC N0000192701 Lymphocyte Function-Associated Antigen-1 Antagonist
CHEBI has role CHEBI:35472 anti-inflammatory drugs
CHEBI has role CHEBI:133024 lymphocyte function-associated antigen-1 antagonists

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Tear film insufficiency indication 46152009




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.42 acidic
pKa2 12.3 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
5% XIIDRA NOVARTIS N208073 July 11, 2016 RX SOLUTION/DROPS OPHTHALMIC 10124000 Nov. 5, 2024 TREATMENT OF THE SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)
5% XIIDRA NOVARTIS N208073 July 11, 2016 RX SOLUTION/DROPS OPHTHALMIC 7745460 Nov. 5, 2024 TREATMENT OF SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)
5% XIIDRA NOVARTIS N208073 July 11, 2016 RX SOLUTION/DROPS OPHTHALMIC 7790743 Nov. 5, 2024 TREATMENT OF SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)
5% XIIDRA NOVARTIS N208073 July 11, 2016 RX SOLUTION/DROPS OPHTHALMIC 8592450 May 17, 2026 TREATMENT OF SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)
5% XIIDRA NOVARTIS N208073 July 11, 2016 RX SOLUTION/DROPS OPHTHALMIC 8367701 April 15, 2029 TREATMENT OF SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)
5% XIIDRA NOVARTIS N208073 July 11, 2016 RX SOLUTION/DROPS OPHTHALMIC 9447077 April 15, 2029 TREATMENT OF THE SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)
5% XIIDRA NOVARTIS N208073 July 11, 2016 RX SOLUTION/DROPS OPHTHALMIC 8168655 May 9, 2029 TREATMENT OF SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Integrin alpha-L/beta-2 Adhesion ANTAGONIST IC50 8.05 SCIENTIFIC LITERATURE DRUG LABEL
Intercellular adhesion molecule 1 Antibody IC50 8.53 CHEMBL

External reference:

IDSource
038E5L962W UNII
D10374 KEGG_DRUG
C3713860 UMLSCUI
CHEBI:133023 CHEBI
CHEMBL2048028 ChEMBL_ID
11965427 PUBCHEM_CID
DB11611 DRUGBANK_ID
CHEMBL2048409 ChEMBL_ID
9584 INN_ID
7533 IUPHAR_LIGAND_ID
1801820 RXNORM
243704 MMSL
31873 MMSL
016935 NDDF
720489009 SNOMEDCT_US
763569006 SNOMEDCT_US
4035938 VANDF
C575157 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Xiidra HUMAN PRESCRIPTION DRUG LABEL 1 0078-0911 SOLUTION/ DROPS 50 mg OPHTHALMIC NDA 24 sections
Xiidra HUMAN PRESCRIPTION DRUG LABEL 1 0078-0911 SOLUTION/ DROPS 50 mg OPHTHALMIC NDA 24 sections
Xiidra HUMAN PRESCRIPTION DRUG LABEL 1 54092-606 SOLUTION/ DROPS 50 mg OPHTHALMIC NDA 23 sections