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 2887.30 38.52 400 6195 454 50598075
Instillation site reaction 2269.66 38.52 300 6295 149 50598380
Eye irritation 1616.36 38.52 386 6209 16754 50581775
Vision blurred 1296.47 38.52 455 6140 78192 50520337
Dysgeusia 749.91 38.52 254 6341 38662 50559867
Instillation site irritation 589.95 38.52 78 6517 37 50598492
Instillation site pruritus 551.75 38.52 71 6524 14 50598515
Instillation site erythema 512.93 38.52 67 6528 23 50598506
Eye pain 466.97 38.52 165 6430 28284 50570245
Instillation site lacrimation 426.37 38.52 54 6541 3 50598526
Ocular hyperaemia 326.23 38.52 116 6479 20176 50578353
Dry eye 271.23 38.52 115 6480 31980 50566549
Lacrimation increased 268.74 38.52 96 6499 16896 50581633
Instillation site discharge 256.78 38.52 33 6562 6 50598523
Eye discharge 252.05 38.52 69 6526 5054 50593475
Instillation site swelling 214.59 38.52 27 6568 0 50598529
Product container issue 207.68 38.52 46 6549 1386 50597143
Eye pruritus 183.80 38.52 67 6528 12467 50586062
Product quality issue 169.72 38.52 82 6513 30776 50567753
Instillation site discomfort 166.89 38.52 21 6574 0 50598529
Ocular discomfort 150.07 38.52 42 6553 3331 50595198
Product use complaint 145.50 38.52 36 6559 1766 50596763
Visual impairment 144.21 38.52 97 6498 68178 50530351
Eye disorder 115.84 38.52 54 6541 18685 50579844
Eyelid margin crusting 92.52 38.52 21 6574 707 50597822
Instillation site dryness 91.91 38.52 12 6583 4 50598525
Product packaging quantity issue 89.32 38.52 22 6573 1058 50597471
Instillation site inflammation 87.41 38.52 11 6584 0 50598529
Foreign body sensation in eyes 78.04 38.52 22 6573 1789 50596740
Eye swelling 77.19 38.52 42 6553 20102 50578427
Instillation site foreign body sensation 76.84 38.52 10 6585 3 50598526
Inappropriate schedule of product administration 76.46 38.52 68 6527 71763 50526766
Taste disorder 74.08 38.52 31 6564 8293 50590236
Instillation site burn 71.52 38.52 9 6586 0 50598529
Superficial injury of eye 69.16 38.52 13 6582 167 50598362
Instillation site hypersensitivity 55.62 38.52 7 6588 0 50598529
Product taste abnormal 48.08 38.52 15 6580 1730 50596799
Instillation site paraesthesia 47.68 38.52 6 6589 0 50598529
Madarosis 46.28 38.52 16 6579 2544 50595985
Product dose omission issue 43.11 38.52 82 6513 183756 50414773
Swelling of eyelid 43.04 38.52 14 6581 1846 50596683

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 603.50 115.31 67 1005 19 29573436
Vision blurred 538.41 115.31 146 926 40030 29533425
Instillation site pain 508.04 115.31 58 1014 37 29573418
Eye irritation 464.05 115.31 91 981 5807 29567648
Lacrimation increased 133.41 115.31 34 1038 6946 29566509
Instillation site lacrimation 129.24 115.31 14 1058 0 29573455

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 2344.18 46.94 292 3184 387 64494869
Instillation site reaction 1830.29 46.94 218 3258 129 64495127
Vision blurred 805.05 46.94 264 3212 90052 64405204
Eye irritation 521.44 46.94 129 3347 15727 64479529
Instillation site irritation 429.45 46.94 50 3426 14 64495242
Instillation site erythema 420.63 46.94 49 3427 14 64495242
Dysgeusia 402.69 46.94 134 3342 46913 64448343
Instillation site pruritus 362.90 46.94 42 3434 9 64495247
Instillation site lacrimation 303.64 46.94 35 3441 6 64495250
Eye pain 192.45 46.94 70 3406 31555 64463701
Instillation site swelling 185.46 46.94 21 3455 0 64495256
Ocular hyperaemia 183.51 46.94 62 3414 22502 64472754
Product quality issue 159.34 46.94 60 3416 29739 64465517
Instillation site discomfort 158.96 46.94 18 3458 0 64495256
Instillation site discharge 158.96 46.94 18 3458 0 64495256
Lacrimation increased 128.08 46.94 45 3431 18301 64476955
Eye discharge 125.54 46.94 33 3443 5051 64490205
Product container issue 111.95 46.94 22 3454 909 64494347
Eye pruritus 84.31 46.94 30 3446 12629 64482627
Instillation site burn 79.47 46.94 9 3467 0 64495256
Visual impairment 75.64 46.94 48 3428 74029 64421227
Instillation site inflammation 70.64 46.94 8 3468 0 64495256
Product dose omission issue 62.62 46.94 64 3412 194683 64300573
Instillation site foreign body sensation 61.81 46.94 7 3469 0 64495256
Inappropriate schedule of product administration 54.94 46.94 43 3433 92243 64403013
Eye swelling 52.18 46.94 25 3451 22256 64473000
Product use complaint 51.95 46.94 13 3463 1633 64493623
Instillation site dryness 50.54 46.94 6 3470 3 64495253

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

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