amlexanox
Trade name: aphthasol
Approved
Dec 17, 1996
Amlexanox is an ant allergic drug, clinically effective for atopic diseases, especially allergic asthma and rhinitis. Amlexanox as a topical paste is a well-tolerated treatment of recurrent aphthous ulcers. Recurrent aphthous ulcer (RAU) is the most prevalent oral mucosal disease in humans, estimated to affect between 5% and 50% of the general population. The mechanism of action by which amlexanox accelerates healing of aphthous ulcers is unknown. In vitro studies have demonstrated amlexanox to be a potent inhibitor of the formation and/or release of inflammatory mediators (histamine and leukotrienes) from mast cells, neutrophils and mononuclear cells. Given orally to animals, amlexanox has demonstrated anti-allergic and anti-inflammatory activities and has been shown to suppress both immediate and delayed type hypersensitivity reactions. The relevance of these activities of amlexanox to its effects on aphthous ulcers has not been established. Amlexanox inhibits chemical mediatory release of the slow-reacting substance of anaphylaxis (SRS-A) and may have antagonistic effects on interleukin-3. When cells are under stress, they release an inactive form of human fibroblast growth factor 1 (FGF-1), a potent mitogen (entity that causes mitosis). Amlexanox binds to FGF1, increasing its conformational stability, sterically blocking Cu(2+) induced oxidation which normally leads to activation of FGF-1. This drug has been discontinued in the U.S — NCATS
Clinical trial activity
3 trials · 4 clinical orgs · 1 marketing orgs
Earliest trial started Feb 1, 2000 (NCT01083875)
Timeline
Indications
Approved for
Mechanism of action
Approval history
- approvedPriority reviewDec 17, 1996
Chemistry & pharmacology
SMILES
CC(C)C1=CC2=C(OC3=NC(N)=C(C=C3C2=O)C(O)=O)C=C1- Mol. weight
- 298.2934 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Topical
- Availability
- Discontinued
Oral
No
Parenteral
No
Topical
Yes
Sources
- WikipediaAmlexanox ↗
- NCATSBRL1C2459K ↗
- ChEMBLCHEMBL1096 ↗
Also known as
- 2-amino-7-isopropyl-5-oxo-5h-(1)benzopyrano(2,3-b)pyridine-3-carboxylic acid
- 2-amino-7-isopropyl-5-oxo-5h-(1)benzopyrano(2,3-b)pyridine-3-carboxylic acid
- 2-amino-7-isopropyl-5-oxo-5h-(1)benzopyrano(2,3b)pyridine-3-carboxylic acid
- 5h-(1)benzopyrano(2,3-b)pyridine-3-carboxylic acid, 2-amino-7-(1-methylethyl)-5-oxo-
- aa 673
- aa-673
- aa-673
- aa-673
- amlenanox
- amlexanox
- amlexanox
- amlexanox
- amlexanox
- amlexanox
- amlexanox
- amlexanox
- amlexanox
- amlexanox
- amlexanox
- amlexanoxo
- amlexanoxo
- amlexanoxum
- amlexanoxum
- amoxanox
- amoxanox
- amoxanox
- amoxanox
- aphthasol
- aphthasol
- aphthasol
- aphthasol
- aphthasol
- aphthasol
- aphthasol
- aphtheal
- chx 3673
- chx-3673
- chx-3673
- glaxosmithkline brand of amlexanox
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT01975935 | Phase 2 | Jan 1, 2014 | University of Michigan |
| NCT01842282 | Phase 2 | Apr 1, 2013 | University of Michigan |
| NCT01083875 | Phase 2 | Feb 1, 2000 | Access Pharmaceuticals, Inc., Advanced Clinical Research Inc., Harvard University |
Organizations
Research & Development (4)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| University of Michigan | Academic/Hospital | 2 | 2 | 1 | 2013 |
| Access Pharmaceuticals, Inc. | For profit | 1 | 1 | 1 | 2000 |
| Advanced Clinical Research Inc. | For profit | 1 | 0 | 1 | 2000 |
| Harvard University | Academic/Hospital | 1 | 0 | 1 | 2000 |