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Oxytocin

Pitocin, Syntocinon

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Studies 93
Trials 100
Completed PHASE1 INTERVENTIONAL NCT02257359

Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Epelsiban in Healthy Female Volunteers

View on ClinicalTrials.gov Updated Dec 15, 2025

Brief Summary

Epelsiban is a potent and selective oxytocin receptor antagonist in development for enhanced implantation rates during in-vitro fertilization (IVF). This study a non-randomized, open label study designed to assess the safety, tolerability and pharmacokinetics of additional repeat doses of epelsiban in healthy females, and will be the first dosing experience of greater than 200 milligram (mg) as a single dose with this compound. Data from this study will inform the selection of doses of epelsiban to be used in future clinical studies. This study will be composed of 3 periods: Screening, Treatment, and Follow-up. The total duration that a subject involved in the study will be up to 6 weeks. At least 2 cohorts of subjects will be enrolled in this study and cohorts will be conducted sequentially. Additional cohorts will be enrolled if determined necessary. A sufficient number of subjects will be screened for the study to obtain approximately 6 evaluable subjects per cohort.

Interventions

Name: Epelsiban
Type: DRUG
Description: Epelsiban will be supplied as a 25 mg white to off-white round direct compression oral tablet.

Primary Outcomes

Measure: Composite pharmacokinetic parameters of epelsiban and its metabolite (GSK2395448)
TimeFrame: Up to Day 2
Description: Pharmacokinetic parameters including area under the plasma drug (and metabolite) concentration versus time curve (AUC\[0-t\], AUC\[0- infinity\], AUC\[0-tau\]), maximum observed concentration (Cmax), time to maximum observed plasma drug (and metabolite) concentration (tmax), and terminal half-life (t1/2), as data permit, will be analyzed. Blood samples for pharmacokinetic analysis will be collected on Day 1 (Morning pre-dose and 0.5hour(hr), 1 hr, 4 hr, 6hr, 8 hr, 12 hr post morning dose; evening pre-dose and 12.5 hr, 13 hr post morning dose) and Day 2 (16 hr and 24 hr post Day 1 morning dose).
Measure: Number of subjects with Adverse events (AEs)
TimeFrame: Up to Day 12
Description: An AE is any untoward medical occurrence in a patient or clinical investigation subject, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product.
Measure: Assessment of clinical observations
TimeFrame: Up to Day 12
Description:
Measure: Assessment of hematology parameters
TimeFrame: Up to Day 12
Description: Hematology parameters include complete blood count with red blood cell indices, white blood cell count differential, hemoglobin, hematocrit and platelet count.
Measure: Assessment of clinical chemistry parameters
TimeFrame: Up to Day 12
Description: Clinical chemistry parameters includes glucose, blood urea, creatinine, sodium, potassium, calcium, total protein, albumin, total bilirubin, direct bilirubin, alkaline phosphatase, alanine aminotransferase and aspartate aminotransferase.
Measure: Assessment of urinalysis by dipstick
TimeFrame: Up to Day 12
Description: Urinalysis includes specific gravity, pH, glucose, protein, blood and ketones by dipstick. If blood or protein is abnormal microscopic examination will be done.
Measure: Assessment of vital sign measurements
TimeFrame: Up to Day 12
Description: Vital sign measurements will include temperature, systolic and diastolic blood pressure and heart rate.
Measure: Assessment of 12-lead electrocardiogram (ECG)
TimeFrame: Up to Day 12
Description: Triplicate 12-lead ECGs will be obtained at each timepoint during the study using an ECG machine that automatically calculates the heart rate and measures PR, QRS, QT, and QTc intervals.
Measure: Assessment of physical examination findings
TimeFrame: Up to Day 12
Description: A physical examination will include, at a minimum, assessment of the cardiovascular, respiratory, gastrointestinal and neurological systems. Height and weight will also be measured

Trial Information

NCT ID

NCT02257359

Status

Completed

Study Type

INTERVENTIONAL

Phases

PHASE1

Sponsor

GlaxoSmithKline

Last Updated

December 15, 2025