Approval Probability 71%
TA Base Rate26%
Adjusted LOA41%
ML RiskLOW_RISK
| NCT ID | Title | Phase | Status | Enrollment | Velocity | Design | Start | Completion | Last Updated | Sites | Countries |
|---|---|---|---|---|---|---|---|---|---|---|---|
| NCT02703181 | Dose Escalation Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of Epelsiban Administered in Repeat Doses in Healthy Women Volunteers | PHASE1 | COMPLETED | 31 | — | — | Jul 9, 2015 | Sep 10, 2015 | Sep 13, 2018 | 1 | United States |
| NCT02257359 | Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Epelsiban in Healthy Female Volunteers | PHASE1 | COMPLETED | 12 | — | — | Dec 18, 2014 | Jan 29, 2015 | Sep 13, 2018 | 1 | United States |
Blood samples were collected for Cohort 1 and 2 on Days 1, 7, and 14 at Pre-dose ante meridiem (AM), Pre Dose post meridiem (PM), Pre- Dose PM2 (second PM dose \[16h\]), 0.5, 1, 2, 6, 8.5, 10, 14, 16.5, 17 and 24 hours post dose. Blood samples were collected for Cohort 3 on Days 1, 7, and 14 at Pre-dose AM, Pre Dose PM, 0.5, 1, 4, 6, 8, 12.5, 13, 16 and 24 hours post dose.
Blood samples were collected for Cohort 1 and 2 on Days 1, 7, and 14 at Pre-dose AM, Pre Dose PM, Pre- Dose PM2 (second PM dose \[16h\]), 0.5, 1, 2, 6, 8.5, 10, 14, 16.5, 17 and 24 hours post dose. Blood samples were collected for Cohort 3 on Days 1, 7, and 14 at Pre-dose AM, Pre Dose PM, 0.5, 1, 4, 6, 8, 12.5, 13, 16 and 24 hours post dose.
Blood samples were collected for Cohort 1 and 2 on Days 1, 7, and 14 at Pre-dose AM, Pre Dose PM, Pre- Dose PM2 (second PM dose \[16h\]), 0.5, 1, 2, 6, 8.5, 10, 14, 16.5, 17 and 24 hours post dose. Blood samples were collected for Cohort 3 on Days 1, 7, and 14 at Pre-dose AM, Pre Dose PM, 0.5, 1, 4, 6, 8, 12.5, 13, 16 and 24 hours post dose.
Blood samples were collected for Cohort 1 and 2 on Days 1, 7, and 14 at Pre-dose AM, Pre Dose PM, Pre- Dose PM2 (second PM dose \[16h\]), 0.5, 1, 2, 6, 8.5, 10, 14, 16.5, 17 and 24 hours post dose. Blood samples were collected for Cohort 3 on Days 1, 7, and 14 at Pre-dose AM, Pre Dose PM, 0.5, 1, 4, 6, 8, 12.5, 13, 16 and 24 hours post dose.
Blood samples were collected for Cohort 1 and 2 on Days 1, 7, and 14 at Pre-dose AM, Pre Dose PM, Pre- Dose PM2 (second PM dose \[16h\]), 0.5, 1, 2, 6, 8.5, 10, 14, 16.5, 17 and 24 hours post dose. Blood samples were collected for Cohort 3 on Days 1, 7, and 14 at Pre-dose AM, Pre Dose PM, 0.5, 1, 4, 6, 8, 12.5, 13, 16 and 24 hours post dose.
Blood samples were collected for Cohort 1 and 2 on Days 1, 7, and 14 at Pre-dose AM, Pre Dose PM, Pre- Dose PM2 (second PM dose \[16h\]), 0.5, 1, 2, 6, 8.5, 10, 14, 16.5, 17 and 24 hours post dose. Blood samples were collected for Cohort 3 on Days 1, 7, and 14 at Pre-dose AM, Pre Dose PM, 0.5, 1, 4, 6, 8, 12.5, 13, 16 and 24 hours post dose.
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.
A complete physical examination will include, at a minimum, assessment of the cardiovascular (CV), respiratory, gastrointestinal and neurological systems. Weight will also be measured and recorded; height will only be measured and recorded at Screening.
12-lead ECGs will be obtained after the subject has rested in the semi-supine position for at least 15 minutes. Triplicate 12-lead ECGs will be obtained at each time point during the study using an ECG machine that automatically calculates the heart rate and measures PR, QRS, QT, and corrected QT (QTc) intervals.
Triplicate readings of systolic and diastolic blood pressure will be obtained at each time point in semi-supine position after five minutes of rest.
Triplicate readings of pulse rate will be obtained at each time point in semi-supine position after five minutes of rest.
Clinical laboratory assessments will include hematology, clinical chemistry and urinalysis.
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).
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.
Hematology parameters include complete blood count with red blood cell indices, white blood cell count differential, hemoglobin, hematocrit and platelet count.
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.
Urinalysis includes specific gravity, pH, glucose, protein, blood and ketones by dipstick. If blood or protein is abnormal microscopic examination will be done.
Vital sign measurements will include temperature, systolic and diastolic blood pressure and heart rate.
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.
A physical examination will include, at a minimum, assessment of the cardiovascular, respiratory, gastrointestinal and neurological systems. Height and weight will also be measured
| Arm | Type | Description |
|---|---|---|
| Cohort 1(600 mg Epelsiban or placebo[every 8 hours]) | EXPERIMENTAL | Each subject will receive 200 mg of epelsiban administered TID (every 8 hours) (total daily dose of 600 mg) or a matching placebo administered every 8 hours. |
| Epelsiban Cohort 1 | EXPERIMENTAL | Subjects will receive 300 mg of epelsiban administered orally twice (every 12 hr) on Day 1 (total daily dose of 600 mg) |
| Epelsiban Cohort 2 | EXPERIMENTAL | Epelsiban dose for Cohort 2 will be determined based on data from Cohort 1, but will not exceed a total daily dose of 900 mg, administered orally in divided doses (450 mg every 12 hrs or 300 mg every 8 hrs). |
| Additional Cohorts TBD (to be decided) | EXPERIMENTAL | Subjects will be enrolled if determined necessary, based on data collected in Epelsiban Cohort 1 and Cohort 2 |
| Name | Type | Description |
|---|---|---|
| Epelsiban (GSK557296) | DRUG | White to off-white 0.270 inches x 0.700 inches oblong film coated tablet containing 25 mg or 100 mg epelsiban. To be swallowed whole with water, not to be chewed. |
| Placebo to match GSK557296 | DRUG | White to off-white 0.270 inches x 0.700 inches oblong film coated Tablet containing placebo. To be swallowed whole with water, not to be chewed. |
| Epelsiban | DRUG | Epelsiban will be supplied as a 25 mg white to off-white round direct compression oral tablet. |
Inclusion Criteria: * Female between 18 and 55 years of age inclusive, at the time of consent * Healthy as determined by the investigator or medically qualified designee based on a medical evaluation including medical history, review of medications previously used, physical examination, laboratory ...