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Lifitegrast

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Lifitegrast
Clinical data
Trade namesXiidra
Other namesSAR-1118
AHFS/Drugs.comxiidra
Routes of
administration		Eye drops
ATC code
  • none
Legal status
Legal status
Identifiers
  • N-{[2-(1-Benzofuran-6-ylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl}-3-(methylsulfonyl)-L-phenylalanine
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.245.695 Edit this at Wikidata
Chemical and physical data
FormulaC29H24Cl2N2O7S
Molar mass615.48 g·mol−1
3D model (JSmol)
  • CS(=O)(=O)c1cccc(c1)C[C@@H](C(=O)O)NC(=O)c2c(cc3c(c2Cl)CCN(C3)C(=O)c4ccc5ccoc5c4)Cl
  • InChI=1S/C29H24Cl2N2O7S/c1-41(38,39)20-4-2-3-16(11-20)12-23(29(36)37)32-27(34)25-22(30)13-19-15-33(9-7-21(19)26(25)31)28(35)18-6-5-17-8-10-40-24(17)14-18/h2-6,8,10-11,13-14,23H,7,9,12,15H2,1H3,(H,32,34)(H,36,37)/t23-/m0/s1
  • Key:JFOZKMSJYSPYLN-QHCPKHFHSA-N

Lifitegrast (trade name Xiidra) is a drug for the treatment of keratoconjunctivitis sicca (dry eye syndrome). It is applied in the form of eye drops.[1]

Adverse effects

Common side effects in clinical trials were eye irritation, discomfort, blurred vision, and dysgeusia (a distortion of the sense of taste).[2]

Pharmacology

Mechanism of action

Lifitegrast inhibits an integrin, lymphocyte function-associated antigen 1 (LFA-1), from binding to intercellular adhesion molecule 1 (ICAM-1). This mechanism down-regulates inflammation mediated by T lymphocytes.[1][3]

History

Lifitegrast was initially designed and developed by SARcode Bioscience[4] which was acquired by Shire in 2013,[5] who submitted a new drug application to the US Food and Drug Administration (FDA) in March 2015. The FDA granted Shire a priority review a month later, and requested additional clinical data, which were supplied in January 2016. The drug was finally approved on 11 July 2016.[6][7]

See also

  • Restasis (ciclosporin eye drops for keratoconjunctivitis sicca)

References

  1. ^ a b Tauber, J (December 2015). "Lifitegrast Ophthalmic Solution 5.0% versus Placebo for Treatment of Dry Eye Disease: Results of the Randomized Phase III OPUS-2 Study". Ophthalmology. 122 (12): 2423–31. doi:10.1016/j.ophtha.2015.08.001. PMID 26365210.
  2. ^ Drugs.com: Patient in formation for xiidra.
  3. ^ Murphy, C. J.; Bentley, E; Miller, P. E.; McIntyre, K; Leatherberry, G; Dubielzig, R; Giuliano, E; Moore, C. P.; Phillips, T. E.; Smith, P. B.; Prescott, E; Miller, J. M.; Thomas, P; Scagliotti, R; Esson, D; Gadek, T; O'Neill, C. A. (2011). "The Pharmacologic Assessment of A Novel Lymphocyte Function-Associated Antigen-1 Antagonist (SAR 1118) for the Treatment of Keratoconjunctivitis Sicca in Dogs". Investigative ophthalmology & visual science. 52 (6): 3174–80. doi:10.1167/iovs.09-5078. PMID 21330663.
  4. ^ Semba, Charles; Gadek, Thomas (2016). "Development of lifitegrast: a novel T-cell inhibitor for the treatment of dry eye disease". Clinical Ophthalmology: 1083. doi:10.2147/OPTH.S110557.{{cite journal}}: CS1 maint: unflagged free DOI (link)
  5. ^ "Shire To Acquire Sarcode Bioscience, Expands Presence In Ophthalmology". 25 March 2013.
  6. ^ "FDA Approves Shire's Xiidra". 11 July 2016.
  7. ^ Drugs.com: Xiidra (lifitegrast) FDA Approval History

Template:Protein and peptide receptor modulators

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