A Study to Evaluate the Pharmacokinetics, Safety and Tolerability of Retosiban (GSK221149) When Dosed With Efavirenz (EFZ)
|ClinicalTrials.gov Identifier: NCT01867996|
Recruitment Status : Completed
First Posted : June 4, 2013
Last Update Posted : May 11, 2017
|Condition or disease||Intervention/treatment||Phase|
|Obstetric Labour, Premature||Drug: Retosiban Drug: EFZ 600 mg||Phase 1|
|Study Type :||Interventional (Clinical Trial)|
|Actual Enrollment :||18 participants|
|Intervention Model:||Single Group Assignment|
|Masking:||None (Open Label)|
|Official Title:||To Evaluate the Pharmacokinetics, Safety and Tolerability of Retosiban (GSK221149) Co-administered With EFAVIRENZ|
|Actual Study Start Date :||June 11, 2013|
|Primary Completion Date :||September 26, 2013|
|Study Completion Date :||September 26, 2013|
Experimental: Retosiban and EFZ
All subjects will receive on Day 1, a 6 mg bolus of retosiban for 5 min, followed by a 6 mg/hr infusion for 12 hrs. On Day 2 a washout day will occur. On Days 3-17, subjects will receive EFZ 600 mg OD dose of in the evening. On Day 18, subjects will receive a 6 mg bolus of retosiban for 5 mins, followed by a 6 mg/hr infusion for 12 hrs plus a 600 mg dose of EFZ.
Retosiban will be supplied as clear colorless solution for infusion (300 mg in 20 mL via). Subject will receive loading dose of 6 mg over 5 min infusion followed by 6 mg/hour infusion for 12 hrs on Day 1 and Day 18.Drug: EFZ 600 mg
EZF 600 mg will be supplied as a yellow, capsular-shaped, film-coated tablet. Subjects will receive EFZ 600mg OD in the evening from Day 3 till Day 18.
- Plasma GSK221149 (parent) and GSK2847065 (metabolite) PK parameters of AUC, Cmax and CL. [ Time Frame: 0, 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, and 24 hours (hrs) after the start of the infusion on Day 1 and Day 18. ]The following PK parameters will be determined after administration of GSK221149 with and without EFZ 600 mg: Area under the plasma concentration-time curve (AUC)- from time zero to time t [AUC(0-t)] and from time zero extrapolated to infinite time [AUC(0-infinity)], maximum observed plasma concentration (Cmax) and clearance (CL). CL will be calculated for parent only.
- Safety and tolerability of administration of GSK221149 with and without EFZ 600 mg as assessed by adverse event, concurrent medication review, clinical laboratory tests, ECG, and vital signs measurements. [ Time Frame: Up to 8 Weeks ]Clinical laboratory tests will include hematology, clinical chemistry and urinalysis parameters. Triplicate 12-lead ECGs will be obtained at the screening visit. Single 12-lead ECGs will be obtained at other time points during the study. Vital sign measurements will include systolic and diastolic blood pressure and pulse rate.
- Plasma GSK221149 and GSK2847065 PK parameters of tmax, tlag and t1/2. [ Time Frame: 0, 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, and 24 hours (hrs) after the start of the infusion on Day 1 and Day 18. ]The following PK parameters will be determined after administration of GSK221149 with and without EFZ 600 mg: time to Cmax (tmax), lag time (tlag), and terminal phase half-life (t1/2). The terminal half-life (t1/2) is defined as the time required for the plasma concentration of drug to reach half of its original concentration.
Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT01867996
|United States, Maryland|
|GSK Investigational Site|
|Baltimore, Maryland, United States, 21225|
|Study Director:||GSK Clinical Trials||GlaxoSmithKline|