epelsiban
Small moleculeexperimental
Epelsiban is an orally bioavailable drug which acts as a selective and potent oxytocin receptor antagonist. It was initially developed by GlaxoSmithKline (GSK) for the treatment of premature ejaculation in men and then as an agent to enhance embryo or blastocyst implantation in women undergoing embryo or blastocyst transfer associated with in vitro fertilization (IVF)., and was also investigated for use in the treatment of adenomyosis. — Wikipedia
Clinical trial activity
7 trials · 1 clinical orgs · 0 marketing orgs
Phase 1
5
Phase 2
2
Phase 3
0
Phase 4
0
Earliest trial started Oct 1, 2007 (NCT00549211)
Timeline
Indications
Mechanism of action
- Oxytocin receptorANTAGONIST
OXTR antagonist
Chemistry & pharmacology
Loading structure…
SMILES
CC[C@H](C)[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)N1CCOCC1)c1ccc(C)nc1C- Mol. weight
- 518.66 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL2037511 ↗
- WikipediaEpelsiban ↗
- ChEMBLCHEMBL2105736 ↗
Also known as
- 3-(2,3-dihydro-1h-inden-2-yl)-1-(1-(2,6-dimethyl-3-pyridinyl)-2-(4-morpholinyl)-2-oxoethyl)-6-(1-methylpropyl)-2,5-piperazinedione
- (3r,6r)-3-(2,3-dihydro-1h-inden-2-yl)-1-((1r)-1-(2,6- dimethylpyridin-3-yl)-2-(morpholin- 4-yl)-2-oxoethyl)-6- ((1s)-1-methylpropyl)piperazine-2,5-dione
- epelsiban
- epelsiban
- epelsiban
- epelsiban
- epelsiban
- epelsiban besylate
- epelsiban besylate
- gsk557296
- gsk557296
- gsk557296
- gsk557296
- gsk557296b
- gsk557296b
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02794467 | Phase 2 | Jul 1, 2016 | GlaxoSmithKline |
| NCT02703181 | Phase 1 | Jul 9, 2015 | GlaxoSmithKline |
| NCT02257359 | Phase 1 | Dec 18, 2014 | GlaxoSmithKline |
| NCT02213029 | Phase 1 | Aug 28, 2014 | GlaxoSmithKline |
| NCT01669083 | Phase 1 | Aug 16, 2012 | GlaxoSmithKline |
| NCT01021553 | Phase 2 | Dec 1, 2009 | GlaxoSmithKline |
| NCT00549211 | Phase 1 | Oct 1, 2007 | GlaxoSmithKline |
Showing 7 of 7 trials
Page 1 / 1
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| GlaxoSmithKline | For profit | 7 | 7 | 2 | 2007 |
1 organizations
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