trihexyphenidyl
Approved
May 13, 1949
Trihexyphenidyl (Artane, Apo-Trihex, Parkin, Pacitane), also known as benzhexol and trihex has been in clinical usage for decades.It is an anticholinergic used in the symptomatic treatment of all etiologic groups of parkinsonism and drug induced extrapyramidal reactions (except tardive dyskinesia). Trihexyphenidyl possesses both anticholinergic and antihistaminic effects, although only the former has been established as therapeutically significant in the management of parkinsonism. Trihexyphenidyl is a selective M1 muscarinic acetylcholine receptor antagonist. It is able to discriminate between the M1 (cortical or neuronal) and the peripheral muscarinic subtypes (cardiac and glandular). Trihexyphenidyl partially blocks cholinergic activity in the CNS, which is responsible for the symptoms of Parkinson's disease. It is also thought to increase the availability of dopamine, a brain chemical that is critical in the initiation and smooth control of voluntary muscle movement. Trihexyphenidyl is indicated for the treatment of parkinson's disease and extrapyramidal reactions caused by drugs. — NCATS
Clinical trial activity
3 trials · 7 clinical orgs · 13 marketing orgs
Earliest trial started Jan 1, 2003 (NCT00122044)
Timeline
1940s
- May 13, 1949
Lederle — Earliest FDA Approval
- May 13, 1949
Lederle — NDA Organization
- May 13, 1949
American Cyanamid — NDA Secondary Org
1970s
- Nov 26, 1974
Watson Pharmaceuticals — Marketing Organization
1980s
- Jul 30, 1982
Vanguard — Marketing Organization
- Apr 7, 1989
Pharm Ventures, Ltd. — Marketing Organization
1990s
- Apr 17, 1997
Pharmaceutical Associates — Marketing Organization
- Dec 24, 1998
Novitium Pharma — Marketing Organization
- Sep 27, 1999
Mikart — Marketing Organization
- Sep 27, 1999
Chartwell Pharmaceuticals — Marketing Organization
2010s
- Nov 17, 2010
Natco Pharma — Marketing Organization
- Jan 1, 2018
Earliest Phase 1 Sponsor(trial)
Indications
Mechanism of action
- Muscarinic acetylcholine receptor M1ANTAGONIST
CHRM1 antagonist
Indicated for Parkinson's disease, M1 likely responsible
Approval history
- approvedMay 13, 1949
Chemistry & pharmacology
SMILES
OC(CCN1CCCCC1)(c1ccccc1)C1CCCCC1- Mol. weight
- 301.47 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL1490 ↗
- WikipediaTrihexyphenidyl ↗
- NCATS6RC5V8B7PO ↗
- ChEMBLCHEMBL1092 ↗
Also known as
- agitane
- apo-trihex
- apo-trihex
- artane
- artane
- artane
- artane
- bentex
- benzhexol
- benzhexol
- benzhexol
- benzhexol hcl
- benzhexol hydrochloride
- benzhexol hydrochloride
- benzhexol hydrochloride
- broflex
- (rs)-1-cyclohexyl-1-phenyl-3-(1-piperidyl)propan-1-ol
- (rs)-1-cyclohexyl-1-phenyl-3-(1-piperidyl)propan-1-ol
- tremin
- tremin
- trihexifenidilo
- trihexifenidilo
- trihexyphenidyl
- trihexyphenidyl
- trihexyphenidyl
- trihexyphenidyl
- trihexyphenidyl
- trihexyphenidyl
- trihexyphenidyl
- trihexyphenidyl
- trihexyphenidyl
- trihexyphenidyl
- trihexyphenidyl
- trihexyphénidyle
- trihexyphénidyle
- trihexyphenidyl hcl
- trihexyphenidyl hcl
- trihexyphenidyl hcl
- trihexyphenidyl hydrochloride
- trihexyphenidyl hydrochloride
- trihexyphenidyl hydrochloride
- trihexyphenidyl hydrochloride
- trihexyphenidyl hydrochloride
- trihexyphenidylum
- trihexyphenidylum
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03430596 | Early Phase 1 (Phase 1) | Feb 28, 2018 | Jiao Tong University |
| NCT04523935 | Phase 4 | Dec 7, 2005 | Sathbhavana Brain Clinic |
| NCT00122044 | Phase 2 | Jan 1, 2003 | Crowley Carter Foundation, Don and Linda Carter Foundation, Stanford University, United Cerebral Palsy Foundation, University of Southern California |
Organizations
Research & Development (7)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Crowley Carter Foundation | Academic/Hospital | 1 | 0 | 1 | 2003 |
| Don and Linda Carter Foundation | Academic/Hospital | 1 | 0 | 1 | 2003 |
| Jiao Tong University | Academic/Hospital | 1 | 1 | 1 | 2018 |
| Sathbhavana Brain Clinic | Academic/Hospital | 1 | 1 | 1 | 2005 |
| Stanford University | Academic/Hospital | 1 | 0 | 1 | 2003 |
| United Cerebral Palsy Foundation | Academic/Hospital | 1 | 0 | 1 | 2003 |
| University of Southern California | Academic/Hospital | 1 | 1 | 1 | 2003 |
Marketing (14)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| American Cyanamid | For profit | NDA2 | May 13, 1949 |
| Chartwell Pharmaceuticals | For profit | MKTG | Sep 27, 1999 |
| Hikma | For profit | MKTG | Feb 16, 2000 |
| Hikma | For profit | SYN | Feb 16, 2000 |
| Lederle | For profit | NDA | May 13, 1949 |
| Mikart | For profit | MKTG | Sep 27, 1999 |
| NYLOS | For profit | MKTG | — |
| Natco Pharma | For profit | MKTG | Nov 17, 2010 |
| Novitium Pharma | For profit | MKTG | Dec 24, 1998 |
| Pharm Ventures, Ltd. | For profit | MKTG | Apr 7, 1989 |
| Pharmaceutical Associates | For profit | MKTG | Apr 17, 1997 |
| Schering | For profit | MKTG | — |
| Vanguard | For profit | MKTG | Jul 30, 1982 |
| Watson Pharmaceuticals | For profit | MKTG | Nov 26, 1974 |