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Oxytocin antagonist

Atosiban

Atosiban is a synthetic nonapeptide, a desamino-oxytocin analog that competitively antagonizes oxytocin and vasopressin receptors.

By The Peptides Codex Editorial TeamIndividual review date not recorded

Page data last changed: . Chemistry registry snapshot: . Registry refreshes and identity assessments are separate from scientific content review.

Length
9 aa
Class
Oxytocin antagonist
Function
Oxytocin and vasopressin receptor antagonist
Context
Approved (outside the US) to delay preterm labor

A modified oxytocin peptide that blocks rather than triggers uterine contraction.

Also known as: Tractocile

Part of the Foundational & therapeutic peptides cluster

Overview

Atosiban is a synthetic nonapeptide, a desamino-oxytocin analog that competitively antagonizes oxytocin and vasopressin receptors. By blocking oxytocin-driven calcium release in uterine muscle it suppresses contractions, and it is approved in many countries as a tocolytic to delay preterm birth. Content here is educational only.

Source & context

Biological / chemical source: Synthetic desamino-oxytocin nonapeptide analog

Primary research or clinical context: Approved (outside the US) to delay preterm labor

Turning an agonist into a blocker

Modifying key residues of oxytocin converts the natural agonist into a receptor antagonist. Atosiban is a striking example of how targeted substitutions can flip a peptide's pharmacology from activating to blocking its receptor.

Tocolytic role

By quieting uterine oxytocin receptors, atosiban aims to postpone premature delivery during a defined window of pregnancy. Its receptor-selective mechanism is often contrasted with older, less specific tocolytic drugs in obstetric pharmacology.

Sequence

One-letter sequence commonly cited for Atosiban (educational; isoforms and modifications may differ):

XYITNCPXG

XYITNCPXG

X = non-canonical residue (Residue 1 is mercaptopropanoic acid (deamino-cysteine of the natural sequenec of oxytocin), residue 2 is D-Tyr(2Et), residue 8 is ornithine; disulphide bridge between cysteine residue 6 and N-terminal Mpa). X marks a non-canonical residue — see the structure block below. (Plotted as alanine on the wheel.)

Atosiban9 aa · C43H67N11O12S2 · ≈ 994.2 DaPEPTIDESCODEX.COMN-terminus →→ C-terminusX1Y2I3T4N5C6P7X8G9nonpolarpolaracidicbasicGly / Pronon-canonical (X)Hydropathy (Kyte–Doolittle): ▮ hydrophobic (cyan) / ▮ hydrophilic (rose) · Side-chain charge at pH 7: + / −X = non-canonical residue (Residue 1 is mercaptopropanoic acid (deamino-cysteine of the natural sequenec of …
Atosiban — Structure cardDownload SVG
A1Y2I3T4N5C6P7A8G9
Helical wheel projection

Residues plotted ~100° apart around an α-helix — clustering of one color reveals an amphipathic face.

Analyze sequences in the playground →

Structure & chemistry

Molecular identity & reference confidence

Source-supported reference

Reference values are taken from the cited molecular record or curated profile. A database match is not independent laboratory verification; modifications, counter-ions, and formulations can change the measured mass.

Molecular form
Atosiban (source record; form not independently established)
Species
Not established by this molecular identity audit
Termini (N / C)
Not specified / Not specified

Average reference mass

Reference policy updated: 2026-10-05

Molecular formula
C43H67N11O12S2
Average reference mass
≈ 994.2
Status
Approved medicine in at least one jurisdiction (IUPHAR record)
Chemical modifications (IUPHAR record)

Residue 1 is mercaptopropanoic acid (deamino-cysteine of the natural sequenec of oxytocin), residue 2 is D-Tyr(2Et), residue 8 is ornithine; disulphide bridge between cysteine residue 6 and N-terminal Mpa

Identifiers

Chemistry values: IUPHAR/BPS Guide to Pharmacology, PubChem · fetched 2026-10-01.

Clinical development snapshot

ClinicalTrials.gov lists 23 registered studies with “Atosiban” as an intervention (snapshot 2026-09-06). A registry footprint is not evidence of efficacy or approval.

Registered studies
23
Highest phase reached
Phase 4
Active in latest 100
3
Most recent update
2025-12-09
Most recently updated studies
NCTTitlePhaseStatusUpdated
NCT07185230Atosiban in Women With Previous Implantation Failure and Abnormal Uterine ContractionsNot applicablerecruiting2025-12-09
NCT07140237The Effect of Oral Oxytocin and Atosiban on Top-down Attention ( OTAtosiban )Early phase 1recruiting2025-09-08
NCT07093060The Effect of Oral Oxytocin and Atosiban on Social AttentionEarly phase 1recruiting2025-07-30
NCT06537778Perioperative Use of Atosiban for Ultrasound-indicated Cerclage to Reduce Spontaneous Preterm Birth(sPTB)Not applicablecompleted2025-05-22
NCT05693688Atosiban Versus Placebo in the Treatment of Late Threatened Pre-term BirthPhase 4completed2024-07-25
NCT04468568In Utero Repair of Myelomeningocele: Atosiban Versus Terbutaline—completed2022-06-06
See all on ClinicalTrials.gov →
Concentration math

Atosiban — reconstitution calculator

Enter how much peptide is in the vial and how much diluent (e.g. bacteriostatic water) is added. The tool returns the resulting solution concentration — and, for any amount you type, the volume it corresponds to. This is educational arithmetic, not a dosing recommendation.

Reference form: Atosiban (source record; form not independently established)Average reference mass: 994.2 Da

Syringe graduation
Solution concentration
5 mg/mL5,000 mcg/mL
mcg

Enter an amount to see the volume it corresponds to.

Educational concentration mathematics only. This tool does not recommend a dose, amount, or protocol, and nothing here is medical advice. Many peptides are not authorized by Health Canada for human use — see our reconstitution and bacteriostatic-water guides for context.

Open the Atosiban calculator on its own page →

FAQ about Atosiban

What is Atosiban?+

Atosiban is a synthetic nonapeptide, a desamino-oxytocin analog that competitively antagonizes oxytocin and vasopressin receptors. By blocking oxytocin-driven calcium release in uterine muscle it suppresses contractions, and it is approved in many countries as a tocolytic to delay preterm birth. Content here is educational only.

What Canadian product status is recorded for Atosiban?+

Canadian product status for Atosiban has not been verified in this profile. No verified record here does not mean no authorization exists. Status depends on the product, formulation and use; consult Health Canada's product records.

What is the typical length of Atosiban?+

Atosiban is commonly described as approximately 9 amino acids (Oxytocin antagonist).

Related peptides

References & further reading

  1. 1.van der Windt et al. (2025). Atosiban versus placebo for threatened preterm birth (APOSTEL 8): a multicentre, randomised controlled trial. Lancet
  2. 2.Shubert (1995). Atosiban. Clin Obstet Gynecol
  3. 3.Wang et al. (2023). Efficacy of atosiban for repeated embryo implantation failure: A systematic review and meta-analysis. Front Endocrinol (Lausanne)
  4. 4.Hadar et al. (2013). Effect of an oxytocin receptor antagonist (atosiban) on uterine electrical activity. Am J Obstet Gynecol
  5. 5.Saade et al. (2021). Randomized Trials of Retosiban Versus Placebo or Atosiban in Spontaneous Preterm Labor. Am J Perinatol
  6. 6.van Winden et al. (2020). Effects of tocolysis with nifedipine or atosiban on child outcome: follow-up of the APOSTEL III trial. BJOG
  7. 7.Tsatsaris et al. (2004). Atosiban for preterm labour. Drugs
  8. 8.Manning et al. (2001). Design of oxytocin antagonists, which are more selective than atosiban. J Pept Sci
  9. 9.PubChem — compound summary for Atosiban (CID 5311010)
  10. 10.Wikipedia — Atosiban
Disclaimer: Educational content only. Not medical advice. Not instructions for human use. Research peptides and unapproved products may be restricted or illegal to market for human consumption in your jurisdiction. Consult qualified professionals and applicable law.
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