Drug General Information
Drug ID
D09WYL
Former ID
DIB010428
Drug Name
GSK-557296
Synonyms
Epelsiban; Epelsiban besylate; Premature ejaculation therapeutic (oral), GlaxoSmithKline
Drug Type
Small molecular drug
Indication Premature ejaculation [ICD9: 302.75; ICD10:F52.4] Phase 2 [522869]
Company
GlaxoSmithKline plc
Structure
Download
2D MOL

3D MOL

Formula
C30H38N4O4
Canonical SMILES
C1CN(CCO1)C(=O)[C@H](N1[C@@H](C(=O)N[C@@H](C1=O)C1Cc2c(<br />C1)cccc2)[C@@H](C)CC)c1c(nc(cc1)C)C
PubChem Compound ID
Target and Pathway
Target(s) Oxytocin receptor Target Info Antagonist [532286]
KEGG Pathway Calcium signaling pathway
cAMP signaling pathway
Neuroactive ligand-receptor interaction
Oxytocin signaling pathway
NetPath Pathway TGF_beta_Receptor Signaling Pathway
PANTHER Pathway Oxytocin receptor mediated signaling pathway
Reactome Vasopressin-like receptors
G alpha (q) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Myometrial Relaxation and Contraction Pathways
Oxytocin signaling
Gastrin-CREB signalling pathway via PKC and MAPK
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
Ref 522869ClinicalTrials.gov (NCT01021553) A Study To Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Two Oral Doses of GSK557296 in a Study in Men With Premature Ejaculation. U.S. National Institutes of Health.
Ref 532286Inhibition of ejaculation by the non-peptide oxytocin receptor antagonist GSK557296: a multi-level site of action. Br J Pharmacol. 2013 Aug;169(7):1477-85.

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