CDEK
← All drugs Report issue

lifitegrast

Trade name: xiidra

Small moleculeapproved

Approved

Jul 11, 2016

Lifitegrast (under brand name Xiidra) was approved as an ophthalmic solution for the treatment of the signs and symptoms of dry eye disease. Lifitegrast binds to the integrin lymphocyte function-associated antigen-1 (LFA-1); a cell surface protein found on leukocytes and blocks the interaction of LFA-1 with its cognate ligand intercellular adhesion molecule-1 (ICAM-1). This LFA-1/ICAM-1 interaction is a key step in the inflammatory cascade that contributes to dry eye disease. Besides lifitegrast participates in phase II clinical trials for prevention of the signs and symptoms of allergic conjunctivitis. — NCATS

Clinical trial activity

27 trials · 26 clinical orgs · 10 marketing orgs

Phase 1
3
Phase 2
9
Phase 3
4
Phase 4
14

Earliest trial started Apr 1, 2009 (NCT00882687)

Timeline

2000s

  1. Jul 1, 2008

    SARcode Bioscience — IND Organization

  2. Jul 1, 2008

    SARcode Bioscience — IND Organization

  3. Jan 1, 2009

    Earliest Phase 1 Sponsor(trial)

  4. Jan 1, 2009

    Shire — Earliest Phase 2 Sponsor(trial)

2010s

  1. Jan 1, 2011

    Shire — Earliest Phase 3 Sponsor(trial)

  2. Jul 11, 2016

    Shire — Earliest FDA Approval

  3. Jul 11, 2016

    Novartis — Marketing Organization

  4. Jul 11, 2016

    Shire — NDA Organization

  5. Jul 11, 2016

    Novartis — NDA Secondary Org

  6. Jul 11, 2016

    Bausch & Lomb — Marketing Organization

  7. Jul 27, 2018

    Fresenius — NDA Secondary Org

2020s

  1. Dec 3, 2021

    Auromedics Pharma — Marketing Organization

  2. Jan 11, 2023

    Sun Pharmaceuticals — Marketing Organization

  3. Feb 15, 2023

    Ingenus Pharmaceuticals — Marketing Organization

  4. Aug 4, 2023

    Micro Labs Ltd India — Marketing Organization

  5. Nov 7, 2023

    Eugia Pharma — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewJul 11, 2016

Chemistry & pharmacology

Loading structure…

SMILES

CS(=O)(=O)C1=CC(C[C@H](NC(=O)C2=C(Cl)C3=C(CN(CC3)C(=O)C4=CC5=C(C=CO5)C=C4)C=C2Cl)C(O)=O)=CC=C1
Mol. weight
615.481 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Topical
Availability
Prescription Only

Oral

No

Parenteral

No

Topical

Yes

First in class

Sources

Also known as

  • (2s)-2-(((2-(benzofuran-6-ylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinolin-6- yl)carbonyl)amino)-3-(3-(methylsulfonyl)phenyl)propanoic acid
  • lifitegrast
  • lifitegrast
  • lifitegrast
  • lifitegrast
  • lifitegrast
  • lifitegrast
  • lifitegrast
  • lifitegrast
  • lifitegrast
  • lifitegrast
  • l-phenylalanine, n-((2-(6-benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl)carbonyl)-3-(methylsulfonyl)-
  • sar 1118
  • sar 1118
  • sar 1118
  • sar 1118
  • sar-1118
  • sar-1118
  • sar-1118
  • sar-1118
  • sar 1118-023
  • shp606
  • shp-606
  • xiidra
  • xiidra
  • xiidra
  • xiidra
  • xiidra

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07025811Phase 4Jul 9, 2025Roche
NCT07040826Phase 1Dec 6, 2022Qilu Pharmaceutical Co., Ltd.
NCT05505292Phase 4Sep 22, 2022Novartis, State University of New York
NCT05102409Phase 2Sep 9, 2021Aldeyra Therapeutics, Inc.
NCT04792580Early Phase 1 (Phase 1)Mar 11, 2021Novartis, Yee, Richard W., M.D.
NCT05594745Phase 4Mar 2, 2021Tauber Eye Center
NCT05045053Phase 4Feb 1, 2021Benha University
NCT04734197Phase 2Jan 11, 2021Surface Pharmaceuticals, Inc.
NCT04669561Phase 4Dec 14, 2020Research Insight LLC
NCT04391894Phase 2Sep 10, 2020Novartis
NCT04413253Phase 4Jun 15, 2020Eye Surgeons of Indiana, Ocular Therapeutix, Inc.
NCT04297618Phase 4Jun 1, 2020Novartis, University of Waterloo
NCT04172961Phase 4Jan 1, 2020Sun Pharmaceuticals, Toyos Clinic
NCT04120987Phase 4Sep 25, 2019Bucci Laser Vision Institute
NCT03952481Phase 4Jul 20, 2019Cornell University, Shire
NCT03408015Phase 4Oct 31, 2018Shire, University of Alabama, Birmingham
NCT03431272Phase 4Sep 1, 2018Shire, University of Alabama, Birmingham
NCT04015219N/AJul 18, 2018Tissue Tech Inc.
NCT03686878Phase 4Dec 16, 2016United Therapeutics
NCT03451396Phase 4Dec 12, 2016Lifelong Vision Foundation, Pepose Vision Institute
Showing 20 of 27 trials
Page 1 / 2

Organizations

Research & Development (26)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
ShireFor profit9632009
NovartisFor profit4132020
SARcode BioscienceFor profit4022009
ORA, Inc.For profit2012009
Tauber Eye CenterAcademic/Hospital2122014
University of Alabama, BirminghamAcademic/Hospital2212018
Aldeyra Therapeutics, Inc.For profit1112021
Benha UniversityAcademic/Hospital1112021
Bucci Laser Vision InstituteAcademic/Hospital1112019
Cornell UniversityAcademic/Hospital1112019
Eye Surgeons of IndianaAcademic/Hospital1112020
Johns Hopkins UniversityAcademic/Hospital1112009
Lifelong Vision FoundationAcademic/Hospital1112016
Ocular Therapeutix, Inc.For profit1012020
Pepose Vision InstituteAcademic/Hospital1012016
Qilu Pharmaceutical Co., Ltd.For profit1112022
Research Insight LLCFor profit1112020
RocheFor profit1112025
State University of New YorkAcademic/Hospital1112022
Sun PharmaceuticalsFor profit1012020
26 organizations
Page 1 / 2

Marketing (11)

OrganizationOrg typeRelationshipDate
Auromedics PharmaFor profitMKTGDec 3, 2021
Bausch & LombFor profitMKTGJul 11, 2016
Eugia PharmaFor profitMKTGNov 7, 2023
FreseniusFor profitNDA2Jul 27, 2018
Ingenus PharmaceuticalsFor profitMKTGFeb 15, 2023
Micro Labs Ltd IndiaFor profitMKTGAug 4, 2023
NovartisFor profitMKTGJul 11, 2016
NovartisFor profitNDA2Jul 11, 2016
SARcode BioscienceFor profitINDJul 1, 2008
ShireFor profitNDAJul 11, 2016
Sun PharmaceuticalsFor profitMKTGJan 11, 2023