pimozide
Trade name: orap
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
Earliest trial started Feb 1, 1993 (NCT00004652)
Timeline
1980s
1990s
- Jan 1, 1993
Earliest Phase 2 Sponsor(trial)
2010s
- Jan 1, 2012
Earliest Phase 3 Sponsor(trial)
- Jan 1, 2015
Earliest Phase 1 Sponsor(trial)
- Sep 28, 2015
Par Pharmaceuticals — Marketing Organization
- Sep 28, 2015
Endo Pharmaceuticals — Marketing Organization
- Sep 28, 2015
Bristol-Myers Squibb — Marketing Organization
- Sep 28, 2015
PH HEALTH — Marketing Organization
2020s
- Apr 13, 2026
Novitium Pharma — Marketing Organization
Indications
Approved for
Studied for
- Amyotrophic Lateral Sclerosis · Phase 2
- Anxiety Disorders · Phase 3
- Breast Neoplasms · Phase 1
- Dementia · Phase 3
- Depression · Phase 3
- Intellectual Disability · Phase 2
- Mental Health · Phase 3
- Neoplasms · Phase 2
- Psychophysiologic Disorders · Phase 3
- Psychotic Disorders · Phase 4
- Sarcoma · Phase 1
- Schizophrenia · Phase 4
- Schizophrenia Spectrum and Other Psychotic Disorders · Phase 4
- Tourette Syndrome · Phase 2
Mechanism of action
- Serotonin 2a (5-HT2a) receptorANTAGONIST
HTR2A antagonist
- Dopamine receptorANTAGONIST
Dopamine receptor antagonist
Approval history
- approvedJul 31, 1984
Chemistry & pharmacology
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
- WikipediaPimozide ↗
- NCATS1HIZ4DL86F ↗
- ChEMBLCHEMBL1423 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05507372 | N/A | Oct 1, 2022 | Applied Biology, Inc., Jupiter Wellness, Inc. |
| NCT04529226 | Phase 2 | Sep 30, 2020 | Andalusian Health Service, Fundación Pública Andaluza |
| NCT04993040 | Phase 1 | Apr 22, 2019 | Athenex, Inc., Sun Yat-Sen University |
| NCT03892018 | Phase 1 | Mar 27, 2019 | Athenex, Inc. |
| NCT03544567 | Phase 1 | Jul 31, 2018 | Athenex, Inc. |
| NCT03588039 | Phase 1 | Jul 30, 2018 | Athenex, Inc. |
| NCT03272503 | Phase 2 | Oct 27, 2017 | ALS Canada, Brain Canada, University of Calgary |
| NCT04168957 | Phase 1 | Oct 25, 2017 | Athenex, Inc., PharmaEssentia Corp. |
| NCT03165955 | Phase 1 | May 1, 2017 | Athenex, Inc., PharmaEssentia Corp., Taipei Medical University |
| NCT04180384 | Phase 2 | Sep 23, 2015 | Athenex, Inc., Dunedin Public Hospital, New Zealand |
| NCT04035473 | Phase 1 | Aug 1, 2015 | Athenex, Inc. |
| NCT02463825 | Phase 2 | Apr 1, 2015 | University of Calgary |
| NCT02374567 | Phase 3 | Jan 1, 2015 | Gottfried Wilhelm Leibniz Universität Hannover |
| NCT02307396 | Phase 4 | Nov 1, 2014 | Technical University of Munich |
| NCT01765829 | Phase 3 | Nov 1, 2012 | Government of Spain, Universidad Carlos III Madrid |
| NCT00158223 | Phase 4 | Oct 1, 2004 | Icahn School of Medicine at Mount Sinai, National Institute of Mental Health (NIMH) |
| NCT00374244 | Phase 2 | Jan 1, 2004 | Stanley Medical Research Institute, Yale University |
| NCT00004652 | Phase 2 | Feb 1, 1993 | National Center for Research Resources (NCRR), University of Rochester |
Organizations
Research & Development (22)
Marketing (7)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Bristol-Myers Squibb | For profit | MKTG | Sep 28, 2015 |
| Endo Pharmaceuticals | For profit | MKTG | Sep 28, 2015 |
| Novitium Pharma | For profit | MKTG | Apr 13, 2026 |
| PH HEALTH | For profit | MKTG | Sep 28, 2015 |
| Par Pharmaceuticals | For profit | MKTG | Sep 28, 2015 |
| Teva | For profit | NDA2 | Jul 31, 1984 |
| Teva | For profit | NDA | Jul 31, 1984 |