thioridazine

Trade name: mellaril

Small moleculeapproved

Approved

Mar 15, 1962

Thioridazine (Mellaril or Melleril) is a piperidine typical antipsychotic drug belonging to the phenothiazine drug group and was previously widely used in the treatment of schizophrenia and psychosis. Thioridazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; blocks alpha-adrenergic effect depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis. Thioridazine primary use in medicine was the treatment of schizophrenia. Thioridazine was also tried with some success as a treatment for various psychiatric symptoms seen in people with dementia, but chronic use of thioridazine and other antipsychotics in people with dementia is not recommended. Thioridazine prolongs the QTc interval in a dose-dependent manner. It produces significantly less extrapyramidal side effects than most first-generation antipsychotics. Its use, along with the use of other typical antipsychotics, has been associated with degenerative retinopathies. It has a higher propensity for causing anticholinergic side effects coupled with a lower propensity for causing extrapyramidal side effects and sedation than chlorpromazine but also has a higher incidence of hypotension and cardiotoxicity. It is also known to possess a relatively high liability for causing orthostatic hypotension compared to other antipsychotics. Similarly to other first-generation antipsychotics, it has a relatively high liability for causing prolactin elevation. It is the moderate risk of causing weight gain. — NCATS

Clinical trial activity

5 trials · 8 clinical orgs · 23 marketing orgs

Phase 1
2
Phase 2
1
Phase 3
1
Phase 4
2

Earliest trial started Jun 1, 2013 (NCT01765803)

Timeline

1960s

  1. Mar 15, 1962

    Novartis — Earliest FDA Approval

  2. Mar 15, 1962

    Novartis — NDA Secondary Org

  3. Mar 15, 1962

    Novartis — NDA Organization

1980s

  1. Apr 14, 1983

    Ani Pharmaceuticals — Marketing Organization

  2. Apr 26, 1983

    Alpharma — Marketing Organization

  3. Jul 5, 1983

    Wockhardt — Marketing Organization

  4. Aug 23, 1983

    Actavis — Marketing Organization

  5. Aug 30, 1983

    Fosun — Marketing Organization

  6. Aug 30, 1983

    Chartwell Pharmaceuticals — Marketing Organization

  7. Nov 8, 1983

    Watson Pharmaceuticals — Marketing Organization

  8. Nov 8, 1983

    Teva — Marketing Organization

  9. Nov 8, 1983

    Heritage Pharma — Marketing Organization

  10. Nov 16, 1983

    Mutual Pharmaceutical — Marketing Organization

  11. Nov 18, 1983

    Mylan — Marketing Organization

  12. Nov 18, 1983

    Sun Pharmaceuticals — Marketing Organization

  13. Mar 21, 1984

    Sandoz — Marketing Organization

  14. Jul 2, 1985

    Superpharm — Marketing Organization

  15. Dec 16, 1985

    Roxane Laboratories — Marketing Organization

  16. Dec 16, 1985

    Boehringer Ingelheim — Marketing Organization

1990s

  1. Aug 16, 1996

    Hi Tech Pharmaceuticals — Marketing Organization

  2. Aug 16, 1996

    Akorn, Inc. — Marketing Organization

  3. Aug 16, 1996

    Epic Pharma Llc — Marketing Organization

  4. Aug 28, 1997

    Pharmaceutical Associates — Marketing Organization

2010s

  1. Jan 1, 2013

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2015

    Earliest Phase 3 Sponsor(trial)

Indications

Mechanism of action

Approval history

  • approvedPriority reviewMar 15, 1962

Chemistry & pharmacology

Loading structure…

SMILES

CSc1ccc2c(c1)N(CCC1CCCCN1C)c1ccccc1S2
Mol. weight
370.59 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Racemic Mixture
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Black box warning

Sources

Also known as

  • 10-[2-(1-methyl-2-piperidyl)ethyl]-2-methylsulfanyl-phenothiazine
  • 10-[2-(1-methyl-2-piperidyl)ethyl]-2-methylsulfanyl-phenothiazine
  • 2-methylmercapto-10-(2-(n-methyl-2-piperidyl)ethyl)phenothiazine
  • 2-methylmercapto-10-(2-(n-methyl-2-piperidyl)ethyl)phenothiazine
  • 3-methylmercapto-n-(2'-(n-methyl-2-piperidyl)ethyl)phenothiazine
  • 3-methylmercapto-n-(2'-(n-methyl-2-piperidyl)ethyl)phenothiazine
  • dl-thioridazine
  • malloryl
  • meleril
  • mellaril
  • mellaril
  • mellaril
  • mellaril
  • mellaril-s
  • mellaril-s
  • melleril
  • melleril
  • rideril
  • rideril
  • thioridazin
  • thioridazin
  • thioridazin
  • thioridazine
  • thioridazine
  • thioridazine
  • thioridazine
  • thioridazine
  • thioridazine
  • thioridazine
  • thioridazine
  • thioridazine
  • thioridazine
  • thioridazine
  • thioridazine
  • thioridazine hcl
  • thioridazine hcl
  • thioridazine hcl
  • thioridazine hydrochloride
  • thioridazine hydrochloride
  • thioridazine hydrochloride
  • thioridazine hydrochloride
  • thioridazine hydrochloride intensol
  • thioridazine hydrochloride intensol
  • thioridazinum
  • thioridazinum
  • tioridazina
  • tioridazina
  • tp-21
  • tp-21

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT02435095Phase 4May 1, 2015RWTH Aachen University
NCT02374567Phase 3Jan 1, 2015Gottfried Wilhelm Leibniz Universität Hannover
NCT02307396Phase 4Nov 1, 2014Technical University of Munich
NCT02096289Phase 1Jul 1, 2014Hamilton Health Sciences Corporation, McMaster University
NCT01765803Early Phase 1 (Phase 1)Jun 1, 2013New Mexico Cancer Care Alliance, Oxnard Foundation, University of New Mexico
Showing 5 of 5 trials
Page 1 / 1

Organizations

Research & Development (8)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Gottfried Wilhelm Leibniz Universität HannoverAcademic/Hospital1112015
Hamilton Health Sciences CorporationAcademic/Hospital1012014
McMaster UniversityAcademic/Hospital1112014
New Mexico Cancer Care AllianceAcademic/Hospital1112013
Oxnard FoundationAcademic/Hospital1012013
RWTH Aachen UniversityAcademic/Hospital1112015
Technical University of MunichAcademic/Hospital1112014
University of New MexicoAcademic/Hospital1012013
8 organizations
Page 1 / 1

Marketing (26)

OrganizationOrg typeRelationshipDate
ActavisFor profitMKTGAug 23, 1983
Akorn, Inc.For profitMKTGAug 16, 1996
AlpharmaFor profitMKTGApr 26, 1983
Ani PharmaceuticalsFor profitMKTGApr 14, 1983
Ani PharmaceuticalsFor profitSYNApr 14, 1983
Boehringer IngelheimFor profitMKTGDec 16, 1985
Chartwell PharmaceuticalsFor profitMKTGAug 30, 1983
Epic Pharma LlcFor profitMKTGAug 16, 1996
FosunFor profitMKTGAug 30, 1983
Heritage PharmaFor profitSYNNov 8, 1983
Heritage PharmaFor profitMKTGNov 8, 1983
Hi Tech PharmaceuticalsFor profitMKTGAug 16, 1996
Mutual PharmaceuticalFor profitMKTGNov 16, 1983
MylanFor profitMKTGNov 18, 1983
NovartisFor profitNDA2Mar 15, 1962
NovartisFor profitNDAMar 15, 1962
Par PharmaceuticalsFor profitMKTG
Pharmaceutical AssociatesFor profitMKTGAug 28, 1997
Roxane LaboratoriesFor profitMKTGDec 16, 1985
SandozFor profitMKTGMar 21, 1984
Sun PharmaceuticalsFor profitMKTGNov 18, 1983
SuperpharmFor profitMKTGJul 2, 1985
TevaFor profitMKTGNov 8, 1983
Watson PharmaceuticalsFor profitMKTGNov 8, 1983
West-Ward PharmaceuticalFor profitMKTG
WockhardtFor profitMKTGJul 5, 1983