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: OFP 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: OFP

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)

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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	2908.66	31.32	400	6985	504	63481133
Instillation site reaction	2281.73	31.32	300	7085	182	63481455
Eye irritation	1758.07	31.32	424	6961	21547	63460090
Vision blurred	1337.25	31.32	471	6914	91453	63390184
Dysgeusia	783.01	31.32	267	7118	46443	63435194
Instillation site irritation	594.15	31.32	78	7307	44	63481593
Instillation site pruritus	559.78	31.32	71	7314	14	63481623
Instillation site erythema	514.12	31.32	67	7318	32	63481605
Eye pain	487.29	31.32	173	7212	33681	63447956
Instillation site lacrimation	432.48	31.32	54	7331	3	63481634

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FDA Adverse Event Reporting System (Male)

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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	607.32	98.13	67	1126	19	34955719
Vision blurred	545.29	98.13	150	1043	45813	34909925
Instillation site pain	509.57	98.13	58	1135	40	34955698
Eye irritation	458.47	98.13	93	1100	7468	34948270
Lacrimation increased	138.47	98.13	36	1157	8446	34947292
Instillation site lacrimation	130.08	98.13	14	1179	0	34955738
Eye pain	108.96	98.13	33	1160	13429	34942309
Instillation site erythema	98.78	98.13	11	1182	4	34955734

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FDA Adverse Event Reporting System (Geriatric)

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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	2341.79	39.70	292	3752	431	79739913
Instillation site reaction	1837.58	39.70	218	3826	137	79740207
Vision blurred	821.95	39.70	275	3769	105623	79634721
Eye irritation	558.50	39.70	142	3902	20539	79719805
Instillation site irritation	421.91	39.70	50	3994	29	79740315
Instillation site erythema	416.35	39.70	49	3995	24	79740320
Dysgeusia	411.96	39.70	141	3903	57036	79683308
Instillation site pruritus	365.42	39.70	42	4002	9	79740335
Instillation site lacrimation	305.74	39.70	35	4009	6	79740338
Eye pain	192.01	39.70	72	3972	37506	79702838

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

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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)

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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)

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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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

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External reference:

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ID	Source
016935	NDDF
038E5L962W	UNII
11965427	PUBCHEM_CID
1801820	RXNORM
243704	MMSL
31873	MMSL
4035938	VANDF
720489009	SNOMEDCT_US
7533	IUPHAR_LIGAND_ID
763569006	SNOMEDCT_US

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Pharmaceutical products:

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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	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

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