benfluorex
Benfluorex, sold under the brand name Mediator, is an anorectic and hypolipidemic agent that is structurally related to fenfluramine. It may improve glycemic control and decrease insulin resistance in people with poorly controlled type-2 diabetes. — Wikipedia
Clinical trial activity
1 trials · 7 clinical orgs · 0 marketing orgs
Earliest trial started Oct 1, 2007 (NCT00544518)
Timeline
2000s
- Jan 1, 2007
Earliest Phase 2 Sponsor(trial)
Indications
Studied for
Mechanism of action
SOAT1 inhibitor
Benfluorex and its metabolite have a great affinity for hydrophobic domains such us lipid bilayers. Both compounds can be incorporated into cellular membranes and modify their physical and biological properties. As a consequence they inhibit the activity of several membrane-bound enzymes involved with lipid metabolism: Acyl Coenzyme A: cholesterol-acyltransferase , phosphatidate phosphohydrolase and diacylglycerol acyltransferase. Some in vitro experiments focusing on carbohydrate metabolism have suggested that the antihyperglycemicactivity of benfluorex results from a postinsulin binding effect(s).
High af¿nity to 5-HT2B receptors (TID: 227 / UniProt ID: P41595) with agonist properties on these receptors. This mechanism is responsible for the induce valvular heart disease caused by benfluorex.
Chemistry & pharmacology
SMILES
CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1- Mol. weight
- 351.37 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL400599 ↗
- WikipediaBenfluorex ↗
- ChEMBLCHEMBL1412305 ↗
Also known as
- 1-(2-trifluoromethylphenyl)-2-(benzoyloxyethyl)aminopropane hcl
- 780 se
- benfluorex
- benfluorex
- benfluorex
- benfluorex
- benfluorex
- benfluorex
- benfluorex
- benfluorex
- benfluorex hydrochloride
- benfluorex hydrochloride
- benfluorex hydrochloride, (+-)-isomer
- benfluorex maleate
- benfluorex maleate
- benfluorex methanesulfonate
- benfluorex methanesulfonate
- benfluorex methanesulfonate
- benfluorex methanesulfonate
- benfluorex methanesulfonate
- benfluorex, methanesulfonate salt
- benfluorexum
- benfluorexum
- benfluramate
- benfluramate
- jp 992
- n-(2-benzoyloxyethyl)norfenfluramine
- s 780
- se 780
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT00544518 | Phase 2 | Oct 1, 2007 | Beijing Haijinge medicine Science-tech CO., Bethune International Peace Hospital, Hebei University, Jilin University, People's Liberation Army of China, Shandong Xinhua Pharmaceutical Company, Shanghai University of Traditional Chinese Medicine |
Organizations
Research & Development (7)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Beijing Haijinge medicine Science-tech CO. | Government | 1 | 0 | 1 | 2007 |
| Bethune International Peace Hospital | Academic/Hospital | 1 | 0 | 1 | 2007 |
| Hebei University | Academic/Hospital | 1 | 0 | 1 | 2007 |
| Jilin University | Academic/Hospital | 1 | 0 | 1 | 2007 |
| People's Liberation Army of China | Government | 1 | 1 | 1 | 2007 |
| Shandong Xinhua Pharmaceutical Company | For profit | 1 | 0 | 1 | 2007 |
| Shanghai University of Traditional Chinese Medicine | Academic/Hospital | 1 | 0 | 1 | 2007 |