Lifitegrast

Lifitegrast is a groundbreaking LFA-1 antagonist API and reference standard in ophthalmic medicine, representing the first drug in its class approved for dry eye disease. As a novel T-cell integrin antagonist, Lifitegrast is designed to mimic the binding epitope of ICAM-1, acting as a molecular decoy to block the LFA-1/ICAM-1 interaction and inhibit downstream inflammatory responses. In quality control and regulatory contexts, Lifitegrast is supplied with comprehensive characterization data compliant with regulatory guidelines, making it suitable for analytical method development, method validation (AMV), and quality control applications for ANDA filings. The unique tetrahydroisoquinoline scaffold of Lifitegrast continues to serve as a template for medicinal chemistry research exploring novel integrin antagonists and anti-inflammatory therapeutics.

 

Product Parameters

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Parameter	Specification
Product Name	Lifitegrast
CAS Number	1025967-78-5
Molecular Formula	C₂₉H₂₄Cl₂N₂O₇S
Molecular Weight	615.48 g/mol
Appearance	White solid
Density	1.479±0.06
Melting Point	＞163 °C
Boiling Point	811.9±65.0 °C
Storage Condition	Hygroscopic, -20°C Freezer, Under inert atmosphere

 

Indication

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Lifitegrast is a leukocyte function antigen 1 (LFA-1) antagonist used for the treatment of dry eye syndrome. Lifitegras binds to LFA-1, preventing its interaction with its homologous ligand intercellular adhesion molecule-1 (ICAM-1). ICAM-1 is overexpressed in the corneal and conjunctival tissues of patients with dry eye disease; the binding of LFA-1 to ICAM-1 promotes the formation of immune synapses, thereby facilitating T-cell activation and migration to target tissues. In vitro studies have demonstrated that Lifitegrast inhibits T-cell adhesion to ICAM-1 and suppresses the secretion of inflammatory cytokines in human peripheral blood monocytes. The exact mechanism of Lifitegras in treating dry eye syndrome remains unclear.。

 

Application

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Lifitegrast is a novel small-molecule integrin antagonist that inhibits T cell-mediated inflammation by blocking the interaction between two critical cell surface proteins (lymphocyte function-related antigen 1 and intercellular adhesion molecule 1), thereby mitigating overall inflammatory responses. Lifitegrast strongly suppresses the adhesion of Jurkat T cells to ICAM-1.

 

Bioactivity

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Lifitegrast (SAR1118) is a novel integrin antagonist that inhibits specific T-cell-mediated inflammatory pathways involved in the pathogenesis of DED.

 

Contact Us

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Cosperpharm is your trusted partner for Lifitegrast — from analytical reference standards to commercial API supply. Contact our team today for pricing, documentation, or technical support.