Retosiban, GSK221149A

New Drug Approvals

Retosiban structure.svg

Retosiban, GSK221149A


MW 494.5827, MF C27 H34 N4 O5

Oxytocin antagonist

Threatened pre-term labour


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)​-

Morpholine, 4-[(2R)-[(3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-6-[(1S)-1-methylpropyl]-2,5-dioxo-1-piperazinyl](2-methyl-4-oxazolyl)acetyl]-

Retosiban (GSK-221,149-A)[1][2] is an oral drug which acts as a selective, sub-nanomolar (Ki = 0.65 nM) oxytocin receptorantagonist with >1400-fold selectivity[3] over the related vasopressin receptors and is being developed by GlaxoSmithKline for the treatment of preterm labour.[4][5]

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…

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