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epinastine

Trade name: elestat

Small moleculeapproved

Approved

Oct 16, 2003

Epinastine (brand names Alesion, Elestat, Purivist, Relestat) is a second-generation antihistamine and mast cell stabilizer. Epinastine is a topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from the mast cell. Epinastine is selective for the histamine H1-receptor and has affinity for the histamine H2 receptor. Epinastine also possesses affinity for the α1-, α2-, and 5-HT2 –receptors. Epinastine does not penetrate the blood/brain barrier and, therefore, is not expected to induce side effects of the central nervous system. Elestat ophthalmic solution is indicated for the prevention of itching associated with allergic conjunctivitis. — NCATS

Clinical trial activity

17 trials · 9 clinical orgs · 14 marketing orgs

Phase 1
4
Phase 2
9
Phase 3
7
Phase 4
4

Earliest trial started Nov 1, 1998 (NCT02260063)

Timeline

1990s

  1. Jan 1, 1998

    Earliest Phase 1 Sponsor(trial)

2000s

  1. Jan 1, 2000

    Earliest Phase 3 Sponsor(trial)

  2. Oct 16, 2003

    Allergan — Earliest FDA Approval

  3. Oct 16, 2003

    Allergan — NDA Secondary Org

  4. Oct 16, 2003

    Allergan — NDA Organization

  5. Oct 16, 2003

    GlaxoSmithKline — NDA Secondary Org

  6. Jan 1, 2006

    Earliest Phase 2 Sponsor(trial)

2010s

  1. Jan 27, 2011

    Sandoz — Marketing Organization

  2. Jan 27, 2011

    Novartis — Marketing Organization

  3. Mar 14, 2011

    Esteve Labs — Marketing Organization

  4. Mar 14, 2011

    PHARMOBEDIENT — Marketing Organization

  5. Oct 31, 2011

    Apotex — Marketing Organization

  6. Oct 31, 2011

    Somerset Pharmaceuticals — Marketing Organization

  7. Oct 31, 2011

    Sun Pharmaceuticals — Marketing Organization

  8. Oct 31, 2011

    Mylan — Marketing Organization

  9. Dec 7, 2016

    Chartwell Pharmaceuticals — Marketing Organization

  10. Dec 7, 2016

    CASI Pharmaceuticals, Inc. — Marketing Organization

  11. May 5, 2017

    Akorn, Inc. — Marketing Organization

  12. May 5, 2017

    Epic Pharma Llc — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedOct 16, 2003

Chemistry & pharmacology

Loading structure…

SMILES

NC1=NCC2c3ccccc3Cc3ccccc3N12
Mol. weight
249.32 g/mol
Lipinski Ro5
Pass
Rule of 3
Yes
Chirality
Racemic Mixture
Inorganic
No
Polymer
No
Delivery
Topical
Availability
Prescription Only

Oral

No

Parenteral

No

Topical

Yes

Sources

Also known as

  • 3-amino-9,13b-dihydro-1h-benz(c,f)imidazo(1,5a)azepine
  • 3-amino-9,13b-dihydro-1h-dibenz(c,f)imidazo(1,5-a)azepine
  • 3-amino-9,13b-dihydro-1h-dibenz(c,f)imidazo(1,5-a)azepine
  • alesion
  • alesion
  • alesion
  • alesion
  • alesion
  • alesion
  • de-114
  • de-114
  • elestat
  • elestat
  • elestat
  • epinastin
  • epinastin
  • epinastina
  • epinastina
  • epinastine
  • epinastine
  • epinastine
  • epinastine
  • epinastine
  • epinastine
  • epinastine
  • epinastine
  • epinastine
  • (+-)-epinastine
  • (+-)-epinastine
  • (+/-)-epinastine
  • epinastine hcl
  • epinastine hcl
  • epinastine hcl
  • epinastine hydrochloride
  • epinastine hydrochloride
  • epinastine hydrochloride
  • epinastine hydrochloride
  • epinastine hydrochloride
  • epinastinum
  • epinastinum
  • flurinol
  • relestat
  • relestat
  • relestat
  • wal 80
  • wal 801
  • wal 801
  • wal 801
  • wal801cl
  • wal 801cl
  • wal 801 cl
  • wal-80 cl

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06212973Phase 3Mar 13, 2023Zhaoke (Guangzhou) Pharmaceutical Limited
NCT02251613Phase 4Dec 1, 2013Alcon
NCT01569191Phase 4Mar 1, 2012Aston University, University of Rochester
NCT01363700Phase 3May 30, 2011Santen Inc.
NCT00564421Phase 3Dec 18, 2007Merck
NCT00534794Phase 4Oct 1, 2007Merck, Ophthalmic Consultants of Boston
NCT00489398Phase 4Jul 1, 2007Hom, Milton M., OD, FAAO, Merck
NCT00407927Phase 2Dec 1, 2006Merck
NCT01382654Phase 2Sep 1, 2006Merck
NCT02260050Phase 1Jun 1, 2004Boehringer Ingelheim
NCT02260037Phase 1Aug 1, 2001Boehringer Ingelheim
NCT02182544Phase 3Jun 1, 2001Boehringer Ingelheim
NCT02182557Phase 3Jun 1, 2001Boehringer Ingelheim
NCT02182570Phase 3Jun 1, 2001Boehringer Ingelheim
NCT02182518Phase 3May 1, 2000Boehringer Ingelheim
NCT02182531Phase 1Aug 1, 1999Boehringer Ingelheim
NCT02260063Phase 1Nov 1, 1998Boehringer Ingelheim
Showing 17 of 17 trials
Page 1 / 1

Organizations

Research & Development (9)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Boehringer IngelheimFor profit8821998
MerckFor profit5432006
AlconFor profit1112013
Aston UniversityAcademic/Hospital1112012
Hom, Milton M., OD, FAAOAcademic/Hospital1112007
Ophthalmic Consultants of BostonAcademic/Hospital1012007
Santen Inc.For profit1112011
University of RochesterAcademic/Hospital1012012
Zhaoke (Guangzhou) Pharmaceutical LimitedGovernment1112023
9 organizations
Page 1 / 1

Marketing (16)

OrganizationOrg typeRelationshipDate
Akorn, Inc.For profitMKTGMay 5, 2017
AllerganFor profitNDA2Oct 16, 2003
AllerganFor profitNDAOct 16, 2003
ApotexFor profitMKTGOct 31, 2011
CASI Pharmaceuticals, Inc.For profitMKTGDec 7, 2016
Chartwell PharmaceuticalsFor profitMKTGDec 7, 2016
Epic Pharma LlcFor profitMKTGMay 5, 2017
Esteve LabsFor profitSYNMar 14, 2011
Esteve LabsFor profitMKTGMar 14, 2011
GlaxoSmithKlineFor profitNDA2Oct 16, 2003
MylanFor profitMKTGOct 31, 2011
NovartisFor profitMKTGJan 27, 2011
PHARMOBEDIENTFor profitMKTGMar 14, 2011
SandozFor profitMKTGJan 27, 2011
Somerset PharmaceuticalsFor profitMKTGOct 31, 2011
Sun PharmaceuticalsFor profitMKTGOct 31, 2011