safotibant
Safotibant (INN) also known by the research code LF22-0542 is a non-peptide bradykinin B1 antagonist. It displayed binding Ki values of 0.35 and 6.5 nM at cloned human and mouse B1 receptors, respectively, while having no affinity for either human, mouse, or rat B2 receptors at concentrations up to 10 μM. This means that LF22-0542 is at least 4000 times selective for the B1 receptor over the B2 receptor. Systemic administration of LF22-0542 inhibited acute pain induced by acetic acid, formalin, and a hot plate. It also reversed acute inflammatory pain induced by carrageenan, and persistent inflammatory pain induced by CFA. In a neuropathic pain model, LF22-0542 reversed the thermal hyperalgesia, but not the mechanical hyperalgesia. — Wikipedia
Clinical trial activity
1 trials · 1 clinical orgs · 0 marketing orgs
Earliest trial started May 1, 2011 (NCT01319487)
Timeline
2010s
- Jan 1, 2011
Earliest Phase 2 Sponsor(trial)
Indications
Studied for
Mechanism of action
- Bradykinin B1 receptorANTAGONIST
BDKRB1 antagonist
Chemistry & pharmacology
SMILES
COc1cc(C)c(S(=O)(=O)N(C)CCOCC(=O)N(C)Cc2ccc(C3=NCCN3)cc2)c(C)c1- Mol. weight
- 502.64 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaSafotibant ↗
- ChEMBLCHEMBL1254771 ↗
Also known as
- fov2304
- fov-2304
- fov-2304
- lf22-0542
- lf22-0542
- lf22-0542
- n-((4-(4,5-dihydro-1h-imidazol-2-yl)phenyl)methyl)-2-(2-(((4-methoxy-2,6-dimethylphenyl) sulfonyl)methylamino)ethoxy)-n-methylacetamide, fumarate
- safotibant
- safotibant
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT01319487 | Phase 2 | May 1, 2011 | Fovea Pharmaceuticals |
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Fovea Pharmaceuticals | For profit | 1 | 1 | 1 | 2011 |