retosiban

Small moleculeexperimental

Retosiban also known as GSK-221,149-A is an oral drug which acts as an oxytocin receptor antagonist. It is being developed by GlaxoSmithKline for the treatment of preterm labour. Retosiban has high affinity for the oxytocin receptor and has greater than 1400-fold selectivity over the related vasopressin receptors — Wikipedia

Clinical trial activity

10 trials · 2 clinical orgs · 0 marketing orgs

Phase 1
6
Phase 2
4
Phase 3
3
Phase 4
0

Earliest trial started Oct 1, 2006 (NCT00457925)

Timeline

2000s

  1. Jan 1, 2006

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2007

    Earliest Phase 2 Sponsor(trial)

2010s

  1. Jan 1, 2015

    Earliest Phase 3 Sponsor(trial)

Indications

Mechanism of action

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)c1coc(C)n1
Mol. weight
494.59 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • (3r,6r)-3-indan-2-yl-1-((1r)-1-(2-methyl-1,3-oxazol-4-yl)-2-morpholin-4-yl-2-oxoethyl)-6-((1s)-1-methylpropyl)-2,5-piperazinedione
  • gsk221149
  • gsk221149
  • gsk221149a
  • gsk221149a
  • gsk221149a
  • retosiban
  • retosiban
  • retosiban
  • retosiban
  • retosiban

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT02377466Phase 3Feb 29, 2016GlaxoSmithKline, PPD
NCT02292784Phase 3Jun 1, 2015GlaxoSmithKline, PPD
NCT02377414Phase 1Mar 2, 2015GlaxoSmithKline
NCT02292771Phase 3Mar 1, 2015GlaxoSmithKline, PPD
NCT01867996Phase 1Jun 11, 2013GlaxoSmithKline
NCT01702376Phase 1Oct 3, 2012GlaxoSmithKline
NCT01627587Phase 1Dec 12, 2011GlaxoSmithKline
NCT00404768Phase 2Oct 12, 2007GlaxoSmithKline
NCT00449709Phase 1Mar 1, 2007GlaxoSmithKline
NCT00457925Phase 1Oct 1, 2006GlaxoSmithKline
Showing 10 of 10 trials
Page 1 / 1

Organizations

Research & Development (2)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
GlaxoSmithKlineFor profit101032006
PPDFor profit3012015
2 organizations
Page 1 / 1