MW 494.5827, MF C27 H34 N4 O5
Threatened pre-term labour
PHASE 3 GSK
UNII-GIE06H28OX, GSK 221149A, 820957-38-8,
(3R.6R)-3-(2,3-dihvdro-1 H-inden-2-v0-1 -( R)-1 -(2-methyl-1 ,3-oxazol-4- yl)-2-(4-morpholinyl)-2-oxoethyll-6-r(1S -1-methylpropyn-2.5- piperazinedione
2,5-Piperazinedione, 3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2-methyl-4-oxazolyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]-, (3R,6R)-
Retosiban (GSK-221,149-A) is an oral drug which acts as a selective, sub-nanomolar (Ki = 0.65 nM) oxytocin receptorantagonist with >1400-fold selectivity over the related vasopressin receptors and is being developed by GlaxoSmithKline for the treatment of preterm labour.
Retosibanis an oxytocin (OT) antagonist in phase III clinical trials at GlaxoSmithKline for the prevention of preterm labor. OT antagonism is widely known to inhibit spontaneous uterine contractions.
Retosiban is a diketopiperazine nonpeptide compound with high potency and selectivity for the OT receptor over vasopressin receptors.
This candidate has been shown to block oxytocin-induced…