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	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 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	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 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	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:

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
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:

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