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iloperidone

Trade name: fanapt

Small moleculeapproved

Approved

May 6, 2009

Iloperidone, also known as Fanapt, Fanapta, and previously known as Zomaril, is an atypical antipsychotic for the treatment of schizophrenia. Iloperidone shows high affinity and maximal receptor occupancy for dopamine D2 receptors in the caudate nucleus and putamen of the brains of schizophrenic patients. The improvement in cognition is attributed to iloperidone's high affinity for α adrenergic receptors. Iloperidone also binds with high affinity to serotonin 5-HT2a and dopamine 3 receptors. Iloperidone binds with moderate affinity to dopamine D4, serotonin 5-HT6 and 5-HT7, and norepinephrine NEα1 receptors. Furthermore, iloperidone binds with weak affinity to serotonin 5-HT1A, dopamine D1, and histamine H1 receptors. Iloperidone is indicated for the treatment of acute schizophrenia. — NCATS

Clinical trial activity

39 trials · 38 clinical orgs · 6 marketing orgs

Phase 1
12
Phase 2
19
Phase 3
9
Phase 4
7

Earliest trial started Nov 1, 2005 (NCT00254202)

Timeline

2000s

  1. Jan 1, 2005

    Vanda Pharmaceuticals — Earliest Phase 3 Sponsor(trial)

  2. Jan 1, 2009

    Earliest Phase 2 Sponsor(trial)

  3. May 6, 2009

    Vanda Pharmaceuticals — Earliest FDA Approval

  4. May 6, 2009

    Vanda Pharmaceuticals — NDA Secondary Org

  5. May 6, 2009

    Vanda Pharmaceuticals — NDA Organization

2010s

  1. Jan 1, 2010

    Earliest Phase 1 Sponsor(trial)

  2. Nov 28, 2016

    Inventia Hlthcare — Marketing Organization

  3. Jul 2, 2018

    Alembic — Marketing Organization

  4. Jul 22, 2019

    Taro Pharmaceuticals — Marketing Organization

  5. Jul 22, 2019

    Sun Pharmaceuticals — Marketing Organization

2020s

  1. May 5, 2022

    Lupin — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedMay 6, 2009

Chemistry & pharmacology

Loading structure…

SMILES

COC1=CC(=CC=C1OCCCN2CCC(CC2)C3=NOC4=C3C=CC(F)=C4)C(C)=O
Mol. weight
426.4806 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Black box warning

Sources

Also known as

  • 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1- piperidinyl]propoxy]-3-methoxyphenyl]ethanone
  • 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1- piperidinyl]propoxy]-3-methoxyphenyl]ethanone
  • 4'-(3-(4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino)propoxy)-3'-methoxyacetophenone
  • 4'-(3-(4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino)propoxy)-3'-methoxyacetophenone
  • ethanone, 1-(4-(3-(4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl)propoxy)-3-methoxyphenyl)-
  • fanapt
  • fanapt
  • fanapt
  • fanapt
  • fanapt
  • fanapta
  • fanapta
  • hp 873
  • hp 873
  • hp-873
  • hp-873
  • hp-873
  • hp-873
  • hp-873
  • hp-873
  • iloperidona
  • iloperidona
  • iloperidone
  • iloperidone
  • iloperidone
  • iloperidone
  • iloperidone
  • iloperidone
  • iloperidone
  • iloperidone
  • iloperidone
  • iloperidone
  • iloperidone
  • iloperidonum
  • iloperidonum
  • zomaril
  • zomaril
  • zomaril
  • zomaril

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07090161Phase 2Jul 28, 2025Vanda Pharmaceuticals
NCT06961968Phase 3May 14, 2025Vanda Pharmaceuticals
NCT06494397Phase 1Jul 31, 2024Vanda Pharmaceuticals
NCT05648591Phase 4Dec 31, 2022Vanda Pharmaceuticals
NCT05344365Phase 2Jun 30, 2022Vanda Pharmaceuticals
NCT04969211Phase 1Jun 30, 2021Vanda Pharmaceuticals
NCT04819776Phase 3Mar 22, 2021Vanda Pharmaceuticals
NCT04712734Phase 1Jan 13, 2021Vanda Pharmaceuticals
NCT04127058Phase 1Oct 7, 2019Vanda Pharmaceuticals
NCT03420534Phase 1Nov 17, 2017Shijiazhuang Pharma Group (CSPC)
NCT03051685Phase 1Jul 20, 2015Dr. Reddy's Laboratories
NCT02404389Phase 2Mar 1, 2015Novartis
NCT02302443Phase 1Feb 1, 2015Hanmi Pharmaceutical
NCT02243046Phase 2Dec 1, 2014Colgate Palmolive
NCT02224625Phase 3Aug 1, 2014Bio-Science Laboratories, Medline Industries
NCT02181803Phase 1Aug 1, 2014Merck
NCT01982916Phase 3Dec 1, 2013Ahn-Gook Pharmaceuticals Co.,Ltd, Catholic University of Korea, Inha University, Konkuk University, Kyung Hee University, Seoul National University, Sungkyunkwan University, Yonsei University
NCT02453893Phase 3Nov 1, 2013Jiao Tong University, Shijiazhuang Pharma Group (CSPC)
NCT01917318Phase 2Jul 1, 2013Novartis, University of Colorado, University of Colorado, Denver
NCT01921712Phase 1Jul 1, 2013Pulmatrix Inc., Quotient
Showing 20 of 39 trials
Page 1 / 2

Organizations

Research & Development (38)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Vanda PharmaceuticalsFor profit131242005
NovartisFor profit12542010
Asahi Kasei PharmaFor profit2212009
Northwestern UniversityAcademic/Hospital2222010
Shijiazhuang Pharma Group (CSPC)For profit2222013
Ahn-Gook Pharmaceuticals Co.,LtdFor profit1112013
Bio-Science LaboratoriesFor profit1012014
Catholic University of KoreaAcademic/Hospital1012013
Colgate PalmoliveFor profit1112014
Columbia UniversityAcademic/Hospital1112012
Dr. Reddy's LaboratoriesFor profit1112015
Hanmi PharmaceuticalFor profit1112015
Harvard UniversityAcademic/Hospital1112012
Inha UniversityAcademic/Hospital1012013
Jiangsu Hansoh Pharmaceutical Co., Ltd.For profit1112012
Jiao Tong UniversityAcademic/Hospital1012013
Johns Hopkins UniversityAcademic/Hospital1112009
Konkuk UniversityAcademic/Hospital1012013
Kyung Hee UniversityAcademic/Hospital1012013
MannKind CorpFor profit1112006
38 organizations
Page 1 / 2

Marketing (10)

OrganizationOrg typeRelationshipDate
AlembicFor profitMKTGJul 2, 2018
Inventia HlthcareFor profitMKTGNov 28, 2016
Inventia HlthcareFor profitSYNNov 28, 2016
LupinFor profitMKTGMay 5, 2022
LupinFor profitSYNMay 5, 2022
Sun PharmaceuticalsFor profitMKTGJul 22, 2019
Taro PharmaceuticalsFor profitSYNJul 22, 2019
Taro PharmaceuticalsFor profitMKTGJul 22, 2019
Vanda PharmaceuticalsFor profitNDA2May 6, 2009
Vanda PharmaceuticalsFor profitNDAMay 6, 2009