Oxetacaine
Oxethazaine is a potent local anesthetic. It is administered orally (usually in combination with an antacid) for the relief of pain associated with peptic ulcer disease or esophagitis. Its effectiveness at the acidity of the gastric environment is due to the fact that oxethazaine, a weak base, is relatively non-ionized at pH 1. It is also used topically in the management of hemorrhoid pain. Oral oxetacaine preparations are available in several countries, including India, South Africa and Brazil, but not the United States. It is marketed under the name Strocain in Japan. — NCATS
Clinical trial activity
1 trials · 5 clinical orgs · 0 marketing orgs
Earliest trial started Apr 1, 2011 (NCT01336530)
Timeline
2010s
- Jan 1, 2011
Earliest Phase 3 Sponsor(trial)
Indications
Studied for
Mechanism of action
- Voltage-gated sodium channelINHIBITOR
Voltage-gated sodium channel inhibitor
- Sodium channel protein type 11 subunit alpha (Scn11a) ↗
- Sodium channel protein type 8 subunit alpha (Scn8a) ↗
- Sodium channel protein type 9 subunit alpha (Scn9a) ↗
- Sodium channel protein type 2 subunit alpha (Scn2a) ↗
- Sodium channel protein type 4 subunit alpha (Scn4a) ↗
- Sodium channel protein type 5 subunit alpha (Scn5a) ↗
- Sodium channel protein type 10 subunit alpha (Scn10a) ↗
- Sodium channel protein type 1 subunit alpha (Scn1a) ↗
- Sodium channel protein (Scn7a) ↗
- Sodium channel protein type 3 subunit alpha (Scn3a) ↗
- Sodium channel protein type 7 subunit alpha ↗
- Sodium channel protein type I alpha subunit
- Sodium channel protein type II alpha subunit
- Sodium channel protein type III alpha subunit
- Sodium channel protein type IX alpha subunit
- Sodium channel protein type XI alpha subunit
- Sodium channel protein type VIII alpha subunit
- Sodium channel protein type X alpha subunit
- Sodium channel protein type IV alpha subunit
- Sodium channel protein type V alpha subunit
- Sodium channel alpha subunits; brain (Types I, II, III)
Chemistry & pharmacology
SMILES
CN(C(=O)CN(CCO)CC(=O)N(C)C(C)(C)CC1=CC=CC=C1)C(C)(C)CC2=CC=CC=C2- Mol. weight
- 467.6434 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- NCATSIP8QT76V17 ↗
- ChEMBLCHEMBL127592 ↗
Also known as
- 2,2'-((2-hydroxyethyl)imino)bis(n-alpha,alpha-dimethylphenethyl)-n-methylacetamide
- mucaine
- mucoxin
- muthesa
- oxaine
- oxaine
- oxetacain
- oxetacaine
- oxetacaine
- oxetacaine
- oxetacaine
- oxetacaine
- oxetacaine
- oxethazaine
- oxethazaine
- oxethazaine
- oxethazaine
- oxethazaine
- oxethazaine hydrochloride
- oxethazaine monohydrochloride
- oxethazine
- robercain r
- storocain
- storocaine
- strocain
- tepilta
- wy-806
- wy-806
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT01336530 | Phase 3 | Apr 1, 2011 | Clinipace LTD, Gottfried Wilhelm Leibniz Universität Hannover, ICON, Meda, Trium Analysis Online GmbH |
Organizations
Research & Development (5)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Clinipace LTD | For profit | 1 | 0 | 1 | 2011 |
| Gottfried Wilhelm Leibniz Universität Hannover | Academic/Hospital | 1 | 0 | 1 | 2011 |
| ICON | For profit | 1 | 0 | 1 | 2011 |
| Meda | For profit | 1 | 1 | 1 | 2011 |
| Trium Analysis Online GmbH | For profit | 1 | 0 | 1 | 2011 |