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paliperidone

Trade name: invega

Small moleculeapproved

Approved

Dec 19, 2006

Paliperidone (9-OH-risperidone) is the primary active metabolite of the older antipsychotic risperidone. While its specific mechanism of action is unknown, it is believed that paliperidone and risperidone act via similar if not the same pathways. It has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism. Paliperidone is also active as an antagonist at alpha 1 and alpha 2 adrenergic receptors and H1 histaminergic receptors, which may explain some of the other effects of the drug. Paliperidone was approved by the FDA for treatment of schizophrenia on December 20, 2006. Very common adverse effects are: headache, tachycardia, somnolence and insomnia. — NCATS

Clinical trial activity

168 trials · 63 clinical orgs · 24 marketing orgs

Phase 1
41
Phase 2
68
Phase 3
59
Phase 4
55

Earliest trial started Mar 1, 2003 (NCT00791232)

Timeline

2000s

  1. Jan 1, 2003

    Johnson and Johnson — Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2003

    Johnson and Johnson — Earliest Phase 2 Sponsor(trial)

  3. Jan 1, 2003

    Johnson and Johnson — Earliest Phase 3 Sponsor(trial)

  4. Dec 19, 2006

    Johnson and Johnson — Earliest FDA Approval

  5. Dec 19, 2006

    Johnson and Johnson — NDA Secondary Org

  6. Dec 19, 2006

    Johnson and Johnson — NDA Organization

2010s

  1. Aug 3, 2015

    Actavis — Marketing Organization

  2. Aug 3, 2015

    Allergan PLC (2015) — Marketing Organization

  3. Sep 24, 2015

    Mylan — Marketing Organization

  4. Sep 24, 2015

    Apicore — Marketing Organization

  5. Apr 6, 2018

    Sun Pharmaceuticals — Marketing Organization

  6. Jun 12, 2019

    Inventia Hlthcare — Marketing Organization

  7. Sep 23, 2019

    Amneal Pharmaceuticals — Marketing Organization

2020s

  1. Oct 29, 2020

    Shijiazhuang Pharma Group (CSPC) — Marketing Organization

  2. Jul 6, 2021

    Teva — Marketing Organization

  3. Jun 29, 2022

    Lupin — Marketing Organization

  4. Jun 30, 2023

    Tolmar Inc. — Marketing Organization

  5. Aug 23, 2023

    Ascent Pharmahealth — Marketing Organization

  6. Feb 5, 2024

    Pharmasciences — Marketing Organization

  7. Jun 26, 2024

    Ajanta Pharma Ltd — Marketing Organization

  8. Jul 26, 2024

    Luye Pharma — Marketing Organization

  9. Sep 26, 2024

    Alembic — Marketing Organization

  10. Oct 8, 2024

    Zydus Discovery DMCC — Marketing Organization

  11. Feb 19, 2025

    Dr. Reddy's Laboratories — Marketing Organization

  12. May 16, 2025

    Accord Research — Marketing Organization

  13. Sep 4, 2025

    Everest Medicines — Marketing Organization

  14. Sep 4, 2025

    ESKAYEF — Marketing Organization

  15. Jan 26, 2026

    Apotex — Marketing Organization

  16. May 7, 2026

    I3 Pharms — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedDec 19, 2006

Chemistry & pharmacology

Loading structure…

SMILES

CCCCCCCCCCCCCCCC(=O)OC1CCCn2c1nc(C)c(CCN1CCC(c3noc4cc(F)ccc34)CC1)c2=O
Mol. weight
664.91 g/mol
Lipinski Ro5
2 violation(s)
Rule of 3
No
Chirality
Racemic Mixture
Inorganic
No
Polymer
No
Delivery
Parenteral
Availability
Prescription Only

Oral

No

Parenteral

Yes

Topical

No

Black box warningProdrug

Sources

Also known as

  • 9-hydroxyrisperidone
  • 9-hydroxyrisperidone
  • invega
  • invega
  • invega
  • invega
  • invega sustenna
  • invega sustenna
  • invega sustenna
  • paliperdidone
  • paliperidone
  • paliperidone
  • paliperidone
  • paliperidone
  • paliperidone
  • paliperidone
  • paliperidone
  • paliperidone
  • paliperidone
  • paliperidone
  • paliperidone palmitate
  • paliperidone palmitate
  • paliperidone palmitate
  • paliperidone palmitate
  • paliperidone palmitate
  • paliperidone palmitate
  • paliperidone palmitate
  • paliperidone palmitate
  • r092670
  • ro76477
  • ro76477
  • ro76477
  • ro76477
  • ro76477
  • ro 76477
  • ro-76477
  • ro-76477
  • ro-76477
  • ro92670
  • ro-92670
  • ro-92670
  • trevicta
  • trevicta
  • xeplion
  • xeplion
  • xeplion

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07075237Phase 4Oct 31, 2025Nanjing University
NCT07153835Phase 4Sep 1, 2025Sher-E-Bangla Medical College
NCT07268430N/ADec 18, 2023Capital Medical University, CSPC Zhongnuo Pharmaceutical (Shijiazhuang) Co., Ltd.
NCT06060886Phase 4Nov 1, 2023Consorcio Centro de Investigación Biomédica en Red, M.P., Hospital de Mataró, Universidad Carlos III Madrid
NCT05321602Phase 1Sep 8, 2021Luye Pharma
NCT04940039Phase 4Jul 22, 2021Johnson and Johnson
NCT04922593Phase 1Jan 13, 2021Luye Pharma
NCT04572685Phase 1Jan 22, 2020Evolution Research Group, Luye Pharma, National Cancer Institute (NCI)
NCT04072575Phase 3Sep 6, 2019Janssen Pharmaceutica NV
NCT03751488Phase 1Dec 12, 2018Luye Pharma
NCT03485417Phase 2/Phase 3 (Phase 3)Dec 1, 2018North District Hospital, The University of Hong Kong
NCT03713658Phase 4Oct 18, 2018Johnson and Johnson
NCT03510325Phase 4Oct 1, 2018Jiao Tong University
NCT03557931Phase 2Jul 13, 2018Astellas
NCT03425552Phase 1/Phase 2 (Phase 2)Mar 11, 2018Pharmathen S.A., Triumpharma
NCT03345342Phase 3Nov 20, 2017Johnson and Johnson
NCT03345979Phase 3Nov 15, 2017Alkermes
NCT03080194Phase 4Apr 1, 2017Huazhong University of Science and Technology
NCT02918825N/ASep 1, 2016Peking University, Wenzhou Medical University
NCT02713282Phase 3Apr 28, 2016Johnson and Johnson
Showing 20 of 168 trials
Page 1 / 9

Organizations

Research & Development (63)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Johnson and JohnsonFor profit12311742003
Janssen Pharmaceutica NVFor profit28142005
Luye PharmaFor profit4412018
National Institute of Mental Health (NIMH)Government4012006
Peking UniversityAcademic/Hospital3322012
Calo Psychiatric CenterAcademic/Hospital2222008
Central South UniversityAcademic/Hospital2012013
Chonbuk National UniversityAcademic/Hospital2212010
Indiana UniversityAcademic/Hospital2122007
OtsukaFor profit2022010
Seoul National UniversityAcademic/Hospital2212011
University of MarylandAcademic/Hospital2122009
University of MichiganAcademic/Hospital2212013
University of North Carolina at Chapel HillAcademic/Hospital2012009
Yale UniversityAcademic/Hospital2122008
AlkermesFor profit1112017
American Foundation for Suicide PreventionAcademic/Hospital1012010
AstellasFor profit1112018
AstraZenecaFor profit1012010
Capital Medical UniversityAcademic/Hospital1012023
63 organizations
Page 1 / 4

Marketing (32)

OrganizationOrg typeRelationshipDate
Accord ResearchFor profitMKTGMay 16, 2025
ActavisFor profitMKTGAug 3, 2015
Ajanta Pharma LtdFor profitMKTGJun 26, 2024
AlembicFor profitMKTGSep 26, 2024
Allergan PLC (2015)For profitMKTGAug 3, 2015
Amneal PharmaceuticalsFor profitMKTGSep 23, 2019
Amneal PharmaceuticalsFor profitSYNSep 23, 2019
ApicoreFor profitMKTGSep 24, 2015
ApotexFor profitMKTGJan 26, 2026
Ascent PharmahealthFor profitMKTGAug 23, 2023
Dr. Reddy's LaboratoriesFor profitMKTGFeb 19, 2025
ESKAYEFFor profitMKTGSep 4, 2025
Everest MedicinesFor profitMKTGSep 4, 2025
I3 PharmsFor profitMKTGMay 7, 2026
Inventia HlthcareFor profitSYNJun 12, 2019
Inventia HlthcareFor profitMKTGJun 12, 2019
Johnson and JohnsonFor profitSYNDec 19, 2006
Johnson and JohnsonFor profitNDA2Dec 19, 2006
Johnson and JohnsonFor profitNDADec 19, 2006
LupinFor profitMKTGJun 29, 2022
LupinFor profitSYNJun 29, 2022
Luye PharmaFor profitMKTGJul 26, 2024
MylanFor profitMKTGSep 24, 2015
MylanFor profitSYNSep 24, 2015
MylanFor profitSYNDec 3, 2024
PharmasciencesFor profitMKTGFeb 5, 2024
Shijiazhuang Pharma Group (CSPC)For profitMKTGOct 29, 2020
Sun PharmaceuticalsFor profitMKTGApr 6, 2018
Sun PharmaceuticalsFor profitSYNApr 6, 2018
TevaFor profitMKTGJul 6, 2021
Tolmar Inc.For profitMKTGJun 30, 2023
Zydus Discovery DMCCFor profitMKTGOct 8, 2024