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Nolasiban

Pharmaceutical compound From Wikipedia, the free encyclopedia

Nolasiban (INNTooltip International Nonproprietary Name; developmental code names OBE001 and RPN-002), also known previously as erlosiban, is an oxytocin receptor antagonist which is under development for the treatment of female infertility and adenomyosis.[2][3][4][5] It was also under development for the treatment of preterm labor, but development for this indication was discontinued.[2] The drug is a small molecule or non-peptide and is taken orally.[2][4][6]

Other namesErlosiban; OBE-001; OBE001; RPN-002; RPN002
Drug classOxytocin receptor antagonist
Elimination half-life12 hours[1]
CAS Number
Quick facts Clinical data, Other names ...
Nolasiban
Clinical data
Other namesErlosiban; OBE-001; OBE001; RPN-002; RPN002
Drug classOxytocin receptor antagonist
Pharmacokinetic data
Elimination half-life12 hours[1]
Identifiers
  • [(2S,4Z)-2-(hydroxymethyl)-4-methoxyiminopyrrolidin-1-yl]-[4-(2-methylphenyl)phenyl]methanone
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC20H22N2O3
Molar mass338.407 g·mol−1
3D model (JSmol)
  • CC1=CC=CC=C1C2=CC=C(C=C2)C(=O)N3C/C(=N\OC)/C[C@H]3CO
  • InChI=1S/C20H22N2O3/c1-14-5-3-4-6-19(14)15-7-9-16(10-8-15)20(24)22-12-17(21-25-2)11-18(22)13-23/h3-10,18,23H,11-13H2,1-2H3/b21-17-/t18-/m0/s1
  • Key:OLUJSZLBWZWGJT-HGBKYHTQSA-N
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The drug interacts with both the oxytocin receptor (Ki = 52 nM; IC50Tooltip half-maximal inhibitory concentration = 81 nM) and the vasopressin V1A receptor (Ki = 120 nM), whereas findings for the vasopressin V2 receptor were not reported.[4][7] It is of relatively low potency, being used and studied clinically at doses of 900 to 2,400 mg orally.[1]

Nolasiban was first described in the scientific literature by 2015.[8][7] It was originated by Merck Serono and is under development by ObsEva and ReproNovo.[2][3] As of July 2026, the drug is in phase 2 clinical trials for female infertility and phase 1 trials for adenomyosis.[2][3] It was also previously in phase 3 trials in the late 2010s.[2][3][9][4]

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