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

Stem definition	Drug id	CAS RN
integrin antagonists	5174	1025967-78-5

Description:

Molecule	Description
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

Molecule

Description

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:

Date	Agency	Company	Orphan
July 11, 2016	FDA	SHIRE DEV LLC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
Tear film insufficiency	indication	46152009

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.42	acidic
pKa2	12.3	acidic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Integrin alpha-L/beta-2	Adhesion	P20701 P05107	ITAL_HUMAN ITB2_HUMAN	ANTAGONIST	IC50	8.05		SCIENTIFIC LITERATURE	DRUG LABEL
Intercellular adhesion molecule 1	Antibody	P05362	ICAM1_HUMAN		IC50	8.53		CHEMBL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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