Lifitegrast

For research use only.

Catalog No.S3714 Synonyms: SAR1118

Lifitegrast Chemical Structure

CAS No. 1025967-78-5

Lifitegrast is a novel small molecule integrin antagonist that inhibits a specific T cell-mediated inflammatory pathway involved in the pathogenesis of DED.

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Biological Activity

Description Lifitegrast is a novel small molecule integrin antagonist that inhibits a specific T cell-mediated inflammatory pathway involved in the pathogenesis of DED.
Targets
Integrin [1]
()
In vitro

Lifitegrast inhibits release of cytokines, interferon d, tumor necrosis factor alpha (TNF-α), and other interleukins (ILs). It is a novel integrin antagonist which prevents LFA-1/ICAM-1 interaction preventing T-cell activation/recruitment and release of inflammatory mediators, thereby decreasing the inflammatory responses in DED[1].

In vivo In vivo study of lifitegrast as radiolabeled drops in rats demonstrated that it was rapidly distributed in ocular and periocular tissues, cleared by normal tear drainage, and was devoid of systemic side effects. A similar dose tolerability study of lifitegrast in dogs suffering from keratoconjunctivitis sicca proved its efficacy and safety. Lifitegrast is found to be a highly potent drug in various clinical trials as it alleviates both the signs and symptoms of DED, which showed rapid onset of action and good therapeutic efficacy as ophthalmic drops. It protected the corneal surfaces and was well tolerated locally as well as systemically[1].

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (162.47 mM)
Ethanol 20 mg/mL (32.49 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 615.48
Formula

C29H24Cl2N2O7S

CAS No. 1025967-78-5
Storage powder
in solvent
Synonyms SAR1118
Smiles CS(=O)(=O)C1=CC=CC(=C1)CC(C(=O)O)NC(=O)C2=C(C=C3CN(CCC3=C2Cl)C(=O)C4=CC5=C(C=C4)C=CO5)Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03866629 Completed Drug: Lifitegrast Dry Eye MDbackline LLC December 20 2018 --
NCT00936520 Terminated Drug: SAR 1118 0.1%|Drug: SAR 1118 1.0%|Drug: SAR 1118 5.0% Diabetic Macular Edema (DME)|Pars Plana Vitrectomy Johns Hopkins University|SARcode Bioscience August 2009 Phase 1

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Integrin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID