pimozide

Trade name: orap

Small moleculeapproved

Approved

Jul 31, 1984

Pimozide (Orap) is a diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to haloperidol for the suppression of vocal and motor tics in patients with Tourette syndrome. It is not intended as a treatment of first choice nor is it intended for the treatment of tics that are merely annoying or cosmetically troublesome. It should be reserved for use in Tourette’s Disorder patients whose development and/or daily life function is severely compromised by the presence of motor and phonic tics. Evidence supporting approval of pimozide for use in Tourette’s Disorder was obtained in two controlled clinical investigations, which enrolled patients between the ages of 8 and 53 years. Most subjects in the two trials were 12 or older. Pimozide is an orally active antipsychotic drug product, which shares with other antipsychotics the ability to blockade dopaminergic receptors on neurons in the central nervous system. Although its exact mode of action has not been established, the ability of pimozide to suppress motor and phonic tics in Tourette’s Disorder is thought to be a function of its dopaminergic blocking activity. However, receptor blockade is often accompanied by a series of secondary alterations in central dopamine metabolism and function which may contribute to both pimozide’s therapeutic and untoward effects. In addition, pimozide, in common with other antipsychotic drugs, has various effects on other central nervous system receptor systems which are not fully characterized. — NCATS

Clinical trial activity

18 trials · 22 clinical orgs · 6 marketing orgs

Phase 1
7
Phase 2
8
Phase 3
2
Phase 4
2

Earliest trial started Feb 1, 1993 (NCT00004652)

Timeline

1980s

  1. Jul 31, 1984

    Teva — Earliest FDA Approval

  2. Jul 31, 1984

    Teva — NDA Secondary Org

  3. Jul 31, 1984

    Teva — NDA Organization

1990s

  1. Jan 1, 1993

    Earliest Phase 2 Sponsor(trial)

2010s

  1. Jan 1, 2012

    Earliest Phase 3 Sponsor(trial)

  2. Jan 1, 2015

    Earliest Phase 1 Sponsor(trial)

  3. Sep 28, 2015

    Par Pharmaceuticals — Marketing Organization

  4. Sep 28, 2015

    Endo Pharmaceuticals — Marketing Organization

  5. Sep 28, 2015

    Bristol-Myers Squibb — Marketing Organization

  6. Sep 28, 2015

    PH HEALTH — Marketing Organization

2020s

  1. Apr 13, 2026

    Novitium Pharma — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedJul 31, 1984

Chemistry & pharmacology

Loading structure…

SMILES

FC1=CC=C(C=C1)C(CCCN2CCC(CC2)N3C(=O)NC4=C3C=CC=C4)C5=CC=C(F)C=C5
Mol. weight
461.5462 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • mcn-jr-6238
  • mcn-jr-6238
  • orap
  • orap
  • orap
  • pimozida
  • pimozida
  • pimozide
  • pimozide
  • pimozide
  • pimozide
  • pimozide
  • pimozide
  • pimozide
  • pimozide
  • pimozide
  • pimozide
  • pimozide
  • pimozidum
  • pimozidum
  • primozide
  • r6238
  • r-6238
  • r-6238
  • r-6238

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT05507372N/AOct 1, 2022Applied Biology, Inc., Jupiter Wellness, Inc.
NCT04529226Phase 2Sep 30, 2020Andalusian Health Service, Fundación Pública Andaluza
NCT04993040Phase 1Apr 22, 2019Athenex, Inc., Sun Yat-Sen University
NCT03892018Phase 1Mar 27, 2019Athenex, Inc.
NCT03544567Phase 1Jul 31, 2018Athenex, Inc.
NCT03588039Phase 1Jul 30, 2018Athenex, Inc.
NCT03272503Phase 2Oct 27, 2017ALS Canada, Brain Canada, University of Calgary
NCT04168957Phase 1Oct 25, 2017Athenex, Inc., PharmaEssentia Corp.
NCT03165955Phase 1May 1, 2017Athenex, Inc., PharmaEssentia Corp., Taipei Medical University
NCT04180384Phase 2Sep 23, 2015Athenex, Inc., Dunedin Public Hospital, New Zealand
NCT04035473Phase 1Aug 1, 2015Athenex, Inc.
NCT02463825Phase 2Apr 1, 2015University of Calgary
NCT02374567Phase 3Jan 1, 2015Gottfried Wilhelm Leibniz Universität Hannover
NCT02307396Phase 4Nov 1, 2014Technical University of Munich
NCT01765829Phase 3Nov 1, 2012Government of Spain, Universidad Carlos III Madrid
NCT00158223Phase 4Oct 1, 2004Icahn School of Medicine at Mount Sinai, National Institute of Mental Health (NIMH)
NCT00374244Phase 2Jan 1, 2004Stanley Medical Research Institute, Yale University
NCT00004652Phase 2Feb 1, 1993National Center for Research Resources (NCRR), University of Rochester
Showing 18 of 18 trials
Page 1 / 1

Organizations

Research & Development (22)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Athenex, Inc.For profit8822015
PharmaEssentia Corp.For profit2012017
University of CalgaryAcademic/Hospital2212015
ALS CanadaAcademic/Hospital1012017
Andalusian Health ServiceAcademic/Hospital1012020
Applied Biology, Inc.For profit1112022
Brain CanadaAcademic/Hospital1012017
Dunedin Public Hospital, New ZealandAcademic/Hospital1012015
Fundación Pública AndaluzaAcademic/Hospital1112020
Gottfried Wilhelm Leibniz Universität HannoverAcademic/Hospital1112015
Government of SpainGovernment1112012
Icahn School of Medicine at Mount SinaiAcademic/Hospital1112004
Jupiter Wellness, Inc.Academic/Hospital1012022
National Center for Research Resources (NCRR)Government1111993
National Institute of Mental Health (NIMH)Government1012004
Stanley Medical Research InstituteAcademic/Hospital1012004
Sun Yat-Sen UniversityAcademic/Hospital1012019
Taipei Medical UniversityAcademic/Hospital1012017
Technical University of MunichAcademic/Hospital1112014
Universidad Carlos III MadridAcademic/Hospital1012012
22 organizations
Page 1 / 2

Marketing (7)

OrganizationOrg typeRelationshipDate
Bristol-Myers SquibbFor profitMKTGSep 28, 2015
Endo PharmaceuticalsFor profitMKTGSep 28, 2015
Novitium PharmaFor profitMKTGApr 13, 2026
PH HEALTHFor profitMKTGSep 28, 2015
Par PharmaceuticalsFor profitMKTGSep 28, 2015
TevaFor profitNDA2Jul 31, 1984
TevaFor profitNDAJul 31, 1984