benzbromarone
Benzbromarone is a uricosuric agent and non-competitive inhibitor of xanthine oxidase used in the treatment of gout, especially when allopurinol, a first-line treatment, fails or produces intolerable adverse effects. It is structurally related to the antiarrhythmic amiodarone. — Wikipedia
Clinical trial activity
10 trials · 14 clinical orgs · 0 marketing orgs
Earliest trial started Jan 1, 2004 (NCT00422318)
Timeline
Indications
Approved for
Mechanism of action
- Solute carrier family 22 member 12INHIBITOR
SLC22A12 inhibitor
Benzbromarone acts by suppressing uric acid reabsorption via inhibition of the uric acid transporter 1 (URAT1) in renal tubular cells. Benzbromarone (BBR) is an inhibitor of Fatty acid-binding protein 4 (FABP4). This indicates that BBR might be a new potential therapeutic agent for type 2 diabetes. Benzbromarone is a very potent inhibitor of CYP2C9.
Molecular docking and point mutations studies revealed that Ser55, Asp76, and Arg126 are the key residues of Fatty acid-binding protein 4 (FABP4) that bind with benzbromarone.
- Xanthine dehydrogenase/oxidaseINHIBITOR
XDH inhibitor
Chemistry & pharmacology
SMILES
CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1- Mol. weight
- 424.09 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaBenzbromarone ↗
- ChEMBLCHEMBL488093 ↗
- ChEMBLCHEMBL388590 ↗
Also known as
- 2-ethyl-3-(3,5-dibrom-4-hydroxybenzoyl)benzofuran
- 2-ethyl-3-(3,5-dibrom-4-hydroxybenzoyl)benzofuran
- 3,5-dibromo-4-hydroxyphenyl-2-ethyl-3-benzofuranyl ketone
- 3,5-dibromo-4-hydroxyphenyl-2-ethyl-3-benzofuranyl ketone
- azubromaron
- benzbromaron
- benzbromaron
- benzbromaron
- benzbromarone
- benzbromarone
- benzbromarone
- benzbromarone
- benzbromarone
- benzbromarone
- benzbromarone
- benzbromarone
- benzbromarone
- desuric
- desuric
- l-2214
- l-2214
- mj-10061
- mj-10061
- narcaricin mite
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05504083 | Phase 2 | Aug 25, 2022 | Chinese Academy of Medical Sciences, InventisBio Inc. |
| NCT05210517 | Phase 4 | Oct 1, 2020 | Free University of Amsterdam |
| NCT03534037 | Phase 4 | Nov 30, 2018 | Government of Taiwan |
| NCT03185793 | Phase 2 | May 11, 2017 | Hengrui Therapeutics, Inc., Jiao Tong University |
| NCT03100318 | Phase 3 | Apr 1, 2017 | Fuji Yakuhin Co., Ltd., Mochida Pharmaceutical Company, Ltd. |
| NCT02944214 | N/A | Oct 1, 2016 | Huazhong University of Science and Technology |
| NCT02790450 | Phase 2 | Oct 1, 2015 | Ludwig Boltzmann Institute, Medical University of Graz |
| NCT02338323 | N/A | Jan 1, 2015 | Huazhong University of Science and Technology |
| NCT02317861 | Phase 1/Phase 2 (Phase 2) | Dec 1, 2014 | Ardea Biosciences, AstraZeneca |
| NCT00422318 | Phase 4 | Jan 1, 2004 | Tottori University |
Organizations
Research & Development (14)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Huazhong University of Science and Technology | Academic/Hospital | 2 | 2 | 1 | 2015 |
| Ardea Biosciences | For profit | 1 | 0 | 1 | 2014 |
| AstraZeneca | For profit | 1 | 1 | 1 | 2014 |
| Chinese Academy of Medical Sciences | Academic/Hospital | 1 | 0 | 1 | 2022 |
| Free University of Amsterdam | Academic/Hospital | 1 | 1 | 1 | 2020 |
| Fuji Yakuhin Co., Ltd. | For profit | 1 | 1 | 1 | 2017 |
| Government of Taiwan | Government | 1 | 1 | 1 | 2018 |
| Hengrui Therapeutics, Inc. | For profit | 1 | 1 | 1 | 2017 |
| InventisBio Inc. | For profit | 1 | 1 | 1 | 2022 |
| Jiao Tong University | Academic/Hospital | 1 | 0 | 1 | 2017 |
| Ludwig Boltzmann Institute | Academic/Hospital | 1 | 0 | 1 | 2015 |
| Medical University of Graz | Academic/Hospital | 1 | 1 | 1 | 2015 |
| Mochida Pharmaceutical Company, Ltd. | For profit | 1 | 0 | 1 | 2017 |
| Tottori University | Academic/Hospital | 1 | 1 | 1 | 2004 |