terbogrel
Terbogrel (INN) is an experimental drug that has been studied for its potential to prevent the vasoconstricting and platelet-aggregating action of thromboxanes. Terbogrel is an orally available thromboxane A2 receptor antagonist and a thromboxane A synthase inhibitor. The drug was developed by Boehringer Ingelheim. — Wikipedia
Clinical trial activity
5 trials · 1 clinical orgs · 0 marketing orgs
Earliest trial started Mar 1, 1998 (NCT02223000)
Timeline
Indications
Mechanism of action
- Thromboxane A2 receptorANTAGONIST
TBXA2R antagonist
Terbogrel mode of action combines the inhibition of the thromboxane A2 (TxA2) receptor with the inhibition of thromboxane A synthase. This combination not only blocks the formation and action of TxA2, but it also leads to an enhanced local production of antithrombotic prostaglandins. This mechanism provides potent antithrombotic action without affecting systemic haemostasis.
- Thromboxane-A synthaseINHIBITOR
TBXAS1 inhibitor
Terbogrel mode of action combines the inhibition of the thromboxane A2 (TxA2) receptor with the inhibition of thromboxane A synthase. This combination not only blocks the formation and action of TxA2, but it also leads to an enhanced local production of antithrombotic prostaglandins. This mechanism provides potent antithrombotic action without affecting systemic haemostasis.
Chemistry & pharmacology
SMILES
CC(C)(C)N/C(=N\C#N)Nc1cccc(/C(=C\CCCC(=O)O)c2cccnc2)c1- Mol. weight
- 405.5 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaTerbogrel ↗
- ChEMBLCHEMBL281398 ↗
Also known as
- (5e)-6-(m-(3-tert-butyl-2-cyanoguanidino)phenyl)-6-(3-pyridyl)-5-hexenoic acid
- 6-(3-(((cyanoamino)((1,1-dimethylethyl)amino)methylene)amino)phenyl)-6-(3-pyridinyl)hexenoic acid
- bibv 308
- bibv 308
- bibv-308-se
- bibv-308-se
- terbogrel
- terbogrel
- terbogrel
- terbogrel
- terbogrel
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02223013 | Phase 1 | Apr 1, 1999 | Boehringer Ingelheim |
| NCT02222987 | Phase 1 | Feb 1, 1999 | Boehringer Ingelheim |
| NCT02223494 | Phase 2 | Oct 1, 1998 | Boehringer Ingelheim |
| NCT02223481 | Phase 2 | May 1, 1998 | Boehringer Ingelheim |
| NCT02223000 | Phase 1 | Mar 1, 1998 | Boehringer Ingelheim |
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Boehringer Ingelheim | For profit | 5 | 5 | 2 | 1998 |