ubenimex
Ubenimex (INN), also known more commonly as bestatin, is a competitive, reversible protease inhibitor. It is an inhibitor of arginyl aminopeptidase (aminopeptidase B), leukotriene A4 hydrolase (a zinc metalloprotease that displays both epoxide hydrolase and aminopeptidase activities), alanyl aminopeptidase (aminopeptidase M/N), leucyl/cystinyl aminopeptidase (oxytocinase/vasopressinase), and membrane dipeptidase (leukotriene D4 hydrolase). It is being studied for use in the treatment of acute myelocytic leukemia and lymphedema. It is derived from Streptomyces olivoreticuli. Ubenimex has been found to inhibit the enzymatic degradation of oxytocin, vasopressin, enkephalins, and various other peptides and compounds. — Wikipedia
Clinical trial activity
3 trials · 1 clinical orgs · 0 marketing orgs
Earliest trial started Apr 1, 2016 (NCT02664558)
Timeline
2010s
- Jan 1, 2016
Earliest Phase 2 Sponsor(trial)
Indications
Mechanism of action
- Aminopeptidase BINHIBITOR
RNPEP inhibitor
Chemistry & pharmacology
SMILES
CC(C)C[C@H](NC(=O)[C@@H](O)[C@H](N)Cc1ccccc1)C(=O)O- Mol. weight
- 308.38 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaUbenimex ↗
- ChEMBLCHEMBL29292 ↗
Also known as
- (3-amino-2-hydroxy-4-phenylbutanoyl)-l-leucine
- 3-amino-2-hydroxy-4-phenylbutyryl-l-leucine
- bestatin
- bestatin
- bestatin
- bestatin
- bestatin, (d-leu)-(r-(r*,r*))-isomer
- bestatin, (d-leu)-(r-(r*,s*))-isomer
- bestatin, (d-leu)-(s-(r*,s*))-isomer
- bestatin, (l-leu)-(r-(r*,r*))-isomer
- bestatin, (l-leu)-(r-(r*,s*))-isomer
- bestatin, (l-leu)-(s-(r*,r*))-isomer
- bestatin, (l-leu)-(s-(r*,s*))-isomer, hydrochloride
- ubenimex
- ubenimex
- ubenimex
- ubenimex
- ubenimex
- ubenimex
- ubenimex
- ubenimex
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02736149 | Phase 2 | Dec 1, 2016 | Eiger BioPharmaceuticals |
| NCT02700529 | Phase 2 | Jun 1, 2016 | Eiger BioPharmaceuticals |
| NCT02664558 | Phase 2 | Apr 1, 2016 | Eiger BioPharmaceuticals |
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Eiger BioPharmaceuticals | For profit | 3 | 3 | 1 | 2016 |