Chemistry:Nolasiban
Nolasiban (INN; 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.[1][2][3][4] It was also under development for the treatment of preterm labor, but development for this indication was discontinued.[1] The drug is a small molecule or non-peptide and is taken orally.[1][3][5]
The drug interacts with both the oxytocin receptor (Ki = 52 nM; IC50 = 81 nM) and the vasopressin V1A receptor (Ki = 120 nM), whereas findings for the vasopressin V2 receptor were not reported.[3][6] It is of relatively low potency, being used and studied clinically at doses of 900 to 2,400 mg orally.[7]
Nolasiban was first described in the scientific literature by 2015.[8][6] It was originated by Merck Serono and is under development by ObsEva and ReproNovo.[1][2] As of July 2026, the drug is in phase 2 clinical trials for female infertility and phase 1 trials for adenomyosis.[1][2] It was also previously in phase 3 trials in the late 2010s.[1][2][9][3]
See also
- Oxytocin receptor antagonist
- Epelsiban
References
- ↑ 1.0 1.1 1.2 1.3 1.4 1.5 "Nolasiban". 8 July 2026. https://adisinsight.springer.com/drugs/800026606.
- ↑ 2.0 2.1 2.2 2.3 "Delving into the Latest Updates on Erlosiban with Synapse". 10 June 2026. https://synapse.patsnap.com/drug/f11faf85dc46415f8b749b5b34fa1712.
- ↑ 3.0 3.1 3.2 3.3 "The Current Status of Drug Discovery for the Oxytocin Receptor". Oxytocin. Methods in Molecular Biology. 2384. New York, NY: Springer US. 2022. pp. 153–174. doi:10.1007/978-1-0716-1759-5_10. ISBN 978-1-0716-1758-8.
- ↑ "Oxytocin antagonists for assisted reproduction". The Cochrane Database of Systematic Reviews 9 (9). September 2021. doi:10.1002/14651858.CD012375.pub2. PMID 34467530.
- ↑ "Confirmation of the cardiac safety of nolasiban in a randomised cohort of healthy female volunteers". Scientific Reports 11 (1). March 2021. doi:10.1038/s41598-021-85650-3. PMID 33739022. Bibcode: 2021NatSR..11.6404T.
- ↑ 6.0 6.1 "Differential Effects of Oxytocin Receptor Antagonists, Atosiban and Nolasiban, on Oxytocin Receptor-Mediated Signaling in Human Amnion and Myometrium". Molecular Pharmacology 91 (4): 403–415. April 2017. doi:10.1124/mol.116.106013. PMID 28188254.
- ↑ Cite error: Invalid
<ref>tag; no text was provided for refs namedPierzyńskiPohlMarchand2021 - ↑ "Pharmacokinetic interactions of OBE001 and betamethasone in healthy female volunteers". Journal of Clinical Pharmacy and Therapeutics 40 (3): 328–332. June 2015. doi:10.1111/jcpt.12258. PMID 25899007.
- ↑ "A placebo-controlled, randomized, double-blind, phase 3 study assessing ongoing pregnancy rates after single oral administration of a novel oxytocin receptor antagonist, nolasiban, prior to single embryo transfer". Fertility and Sterility 110 (4): e45. 2018. doi:10.1016/j.fertnstert.2018.07.141.
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