Lifitegrast

Lymphocyte Function-Associated Antigen-1 Antagonist — SENSORY ORGANS

Key facts

Lifitegrast is an onp drug in the Lymphocyte Function-Associated Antigen-1 Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 2016. Its mechanism of action is classified as Lymphocyte Function-Associated Antigen-1 Antagonists. DrugCentral lists 2 molecular targets, including ICAM1 and ITGAL|ITGB2. Recorded indications include Tear film insufficiency.

• Approval status: onp (first approved 2016 by the FDA).
• Drug class: Lymphocyte Function-Associated Antigen-1 Antagonist.
• Mechanism of action: Lymphocyte Function-Associated Antigen-1 Antagonists.
• Molecular targets: ICAM1 and ITGAL|ITGB2 (2 listed in DrugCentral).
• Indications: Tear film insufficiency.
• ATC code: S01XA25 (Other ophthalmologicals).
• Molecular formula: C29H24Cl2N2O7S; molecular weight 615.48 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Tear film insufficiency

Mechanism & targets

• Mechanism of action (MoA): Lymphocyte Function-Associated Antigen-1 Antagonists
• Established pharmacologic class: Lymphocyte Function-Associated Antigen-1 Antagonist

Molecular targets (2)

Target	Gene	Action	Activity
Intercellular adhesion molecule 1	ICAM1	unknown	IC50 8.53
Integrin alpha-L/beta-2	ITGAL|ITGB2	antagonist	IC50 8.05

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2016-07-11	FDA	—	SHIRE DEV LLC

ATC classification

ATC code	Therapeutic hierarchy
S01XA25	SENSORY ORGANS › OPHTHALMOLOGICALS › OTHER OPHTHALMOLOGICALS › Other ophthalmologicals

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Instillation site pain	4151.1
Instillation site reaction	3559.8
Eye irritation	2523.4
Vision blurred	2290.8
Dysgeusia	1020.6
Instillation site erythema	801.1
Instillation site pruritus	756.3
Eye pain	754.8
Instillation site irritation	739.1
Instillation site lacrimation	649.1
Ocular hyperaemia	525.1
Lacrimation increased	513.0

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Lifitegrast is on its molecule page.

• Molecular formula: C₂₉H₂₄Cl₂N₂O₇S
• Molecular weight: 615.48 g/mol
• CAS number: 1025967-78-5
• InChIKey: JFOZKMSJYSPYLN-QHCPKHFHSA-N
• PubChem CID: 11965427

CS(=O)(=O)C1=CC=CC(C[C@H](NC(=O)C2=C(Cl)C=C3CN(CCC3=C2Cl)C(=O)C2=CC=C3C=COC3=C2)C(O)=O)=C1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Lifitegrast used for?

DrugCentral lists the following indications for Lifitegrast: Tear film insufficiency.

How does Lifitegrast work?

Lifitegrast is classified as Lymphocyte Function-Associated Antigen-1 Antagonists; its molecular targets in DrugCentral include ICAM1 and ITGAL|ITGB2 (antagonist).

When was Lifitegrast first approved?

Lifitegrast was first approved by the FDA in 2016.

What drug class does Lifitegrast belong to?

Lifitegrast is in the Lymphocyte Function-Associated Antigen-1 Antagonist class.

What is the chemical formula of Lifitegrast?

Lifitegrast has the molecular formula C29H24Cl2N2O7S and a molecular weight of 615.48 g/mol.

Sources

• DrugCentral drug card 5174 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2048028 — compound record and bioactivity
• PubChem CID 11965427 — chemical identifiers
• DrugBank DB11611 — drug record
• FDA UNII 038E5L962W — substance identity
• DailyMed: FDA labels for Lifitegrast — current prescribing information (label search)
• UniProt P05362 (ICAM1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.