dezocine
Trade name: dalgan
Dezocine was discovered and patented by American Home Products Corp. in 1978. Dezocine is a partial opiate drug and was used for pain management under brand name Dalgan. But then usage of this drug was discontinued in US. Dezocine acts as a partial μ-receptor agonist, a κ-receptor antagonist, and a norepinephrine and serotonin reuptake inhibitor (via norepinephrine transporter and serotonin transporter). Dezocine shares the CNS depressant and respiratory depressant effects of opioid analgesics. Dezocine has not been shown to produce clinically significant cardiovascular adverse effects. — NCATS
Clinical trial activity
13 trials · 19 clinical orgs · 2 marketing orgs
Earliest trial started Jul 1, 2014 (NCT02289586)
Timeline
1980s
- Jun 1, 1989
American Home Products — First NDA Organization
- Jun 1, 1989
American Home Products — NDA Organization
2020s
- Jan 1, 2020
Earliest Phase 1 Sponsor(trial)
Indications
Approved for
Mechanism of action
- Kappa opioid receptorANTAGONIST
OPRK1 antagonist
- Mu opioid receptorPARTIAL AGONIST
OPRM partial agonist
Approval history
- approved—
Chemistry & pharmacology
SMILES
C[C@@]12CCCCC[C@@H](CC3=CC=C(O)C=C13)[C@@H]2N- Mol. weight
- 245.3599 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Parenteral
- Availability
- Discontinued
Oral
No
Parenteral
Yes
Topical
No
Sources
- WikipediaDezocine ↗
- NCATSVHX8K5SV4X ↗
- ChEMBLCHEMBL1685 ↗
Also known as
- 13-amino-5,6,7,8,9,10,11,12-octahydro-5-methyl-5,11-methanobenzocyclodecenol
- (-)-13beta-amino-5,6,7,8,9,10,11alpha,12-octahydro-5alpha-methyl-5,11-methanobenzocyclodecen-3-ol
- (-)-13beta-amino-5,6,7,8,9,10,11alpha,12-octahydro-5alpha-methyl-5,11-methanobenzocyclodecen-3-ol
- 5,11-methanobenzocyclodecen-3-ol, 5,6,7,8,9,10,11,12-octahydro-13-amino-5-methyl-
- (-5alpha, 11alpha,13s)-13-amino-5,6,7,8,9,10,11,12-octahydro-5-methyl-5,11-methanobenzocyclodecen-3-ol
- dalgan
- dalgan
- dalgan
- dalgan
- dezocina
- dezocina
- dezocine
- dezocine
- dezocine
- dezocine
- dezocine
- dezocine
- dezocine
- dezocine
- dezocine
- dezocine
- dezocine
- dezocine, (5alpha,11alpha,13s*)-isomer
- dezocine hydrobromide
- dezocine hydrobromide
- dezocine hydrobromide
- dezocine hydrobromide
- dezocine hydrobromide
- dezocine hydrobromide, (5alpha,11alpha,13*)-isomer
- dezocine hydrobromide, (5alpha,11alpha,13s*)-isomer
- dezocine hydrobromide, (5r-(5alpha,11alpha,13s*))-isomer
- dezocine hydrobromide, (5s-(5alpha,11alpha,13*))-isomer
- dezocinum
- dezocinum
- docozine
- wy-16225
- wy-16225
- wy-16,225
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05861063 | Phase 4 | Feb 11, 2023 | Xijing Hospital |
| NCT06439368 | Phase 4 | Jan 5, 2023 | Southern Medical University, Yangtze River Pharmaceutical Group Co., Ltd. |
| NCT05515822 | Phase 4 | Oct 1, 2022 | Sichuan University |
| NCT06000137 | N/A | Feb 10, 2022 | Fudan University |
| NCT04906317 | N/A | Dec 1, 2020 | Sun Yat-Sen University |
| NCT04515953 | Phase 1 | Aug 31, 2020 | Nang Kuang Pharmaceutical Co., Ltd., National Taiwan University |
| NCT04111302 | N/A | Oct 1, 2019 | Chengdu University of Traditional Chinese Medicines |
| NCT03823846 | N/A | Nov 1, 2017 | Zhejiang University |
| NCT03147066 | Phase 4 | Jun 1, 2017 | Southeast University, Zhongda Hospital |
| NCT03014713 | Phase 4 | Sep 1, 2016 | Guangzhou General Hospital of Guangzhou Military Command, People's Liberation Army of China |
| NCT02768168 | N/A | May 1, 2016 | Ningxia Medical University |
| NCT02673723 | Phase 4 | Mar 1, 2016 | Anhui College of Traditional Chinese Medicine, Anhui Medical University |
| NCT02289586 | N/A | Jul 1, 2014 | Futian People's Hospital, Science and Technology Innovation Commission of Shenzhen Municipality |
Organizations
Research & Development (19)
Marketing (2)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| American Home Products | For profit | NDA | Jun 1, 1989 |
| AstraZeneca | For profit | NDA2 | — |