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drug3159 | [14C]-GSK3640254 intravenous infusion Wiki | 1.00 |
drug3160 | [14C]-GSK3640254 powder Wiki | 1.00 |
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There is one clinical trial.
This is an open-label, single-center, single group, non-randomized, two-period, single sequence, mass balance study which will enroll 6 healthy male participants. This study will assess the pharmacokinetics, balance/excretion, and metabolism of GSK3640254 in humans using [14C]-radiolabeled drug substance administered as an intravenous (IV) infusion and via the oral route. The study will also provide an assessment of GSK3640254 absorption, metabolism and excretion following administration of a [14C]-radiolabeled oral suspension. Each participant will be involved in the study for up to 10 weeks which will include a screening period, two treatment periods (treatment Periods 1 and 2) separated by a washout of at least 13 days between oral doses, and a follow-up visit 7-14 days after the last assessment in treatment Period 2.
Description: Blood samples will be collected at the indicated time points to evaluate [14C]-GSK3640254 in plasma.
Measure: Treatment period 1: Area under the concentration-time curve from time zero (pre-dose) extrapolated to infinite time (AUC[0-inf]) in plasma following administration of IV dose of 14 Carbon [14C]-GSK3640254 Time: Day 1 (Pre-dose, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate GSK3640254 in plasma.
Measure: Treatment period 1: AUC(0-inf) in plasma following administration of oral dose of GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate total radioactivity in plasma.
Measure: Treatment period 1: AUC(0-inf) of total radioactivity in plasma following administration of IV dose of [14C]-GSK3640254 Time: Screening, Day-1, Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate GSK3640254 in plasma.
Measure: Treatment period 2: AUC(0-inf) in plasma following administration of oral dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate total radioactivity in plasma.
Measure: Treatment period 2: AUC(0-inf) of total radioactivity in plasma following administration of oral dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate [14C]-GSK3640254 in plasma.
Measure: Treatment period 1: AUC from time zero (pre-dose) to last time of quantifiable concentration within a participant across all treatments (AUC[0-t]) in plasma following administration of IV dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate GSK3640254 in plasma.
Measure: Treatment period 1: AUC (0-t) in plasma following administration of oral dose of GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate total radioactivity in plasma.
Measure: Treatment period 1: AUC(0-t) of total radioactivity in plasma following administration of IV dose of [14C]-GSK3640254 Time: Screening, Day-1, Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate GSK3640254 in plasma.
Measure: Treatment period 2: AUC (0-t) in plasma following administration of oral dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate total radioactivity in plasma.
Measure: Treatment period 2: AUC(0-t) of total radioactivity in plasma following administration of oral dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate [14C]-GSK3640254 in plasma.
Measure: Treatment period 1: Maximum observed concentration (Cmax) in plasma following administration of IV dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate GSK3640254 in plasma.
Measure: Treatment period 1:Cmax in plasma following administration of oral dose of GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate total radioactivity in plasma.
Measure: Treatment period 1: Cmax of total radioactivity in plasma following administration of IV dose of [14C]-GSK3640254 Time: Screening, Day-1, Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate GSK3640254 in plasma.
Measure: Treatment period 2: Cmax in plasma following administration of oral dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-doseDescription: Blood samples will be collected at the indicated time points to evaluate total radioactivity in plasma.
Measure: Treatment period 2: Cmax of total radioactivity in plasma following administration of oral dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate total radioactivity in blood.
Measure: Treatment period 2: Cmax of total radioactivity in blood following administration of oral dose of [14C]-GSK3640254 Time: Day 1 (2, 4, 6, 8, 10 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate [14C]-GSK3640254 in plasma.
Measure: Treatment period 1:Time of occurrence of Cmax (Tmax) in plasma following administration of IV dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate GSK3640254 in plasma.
Measure: Treatment period 1:Tmax in plasma following administration of oral dose of GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate total radioactivity in plasma.
Measure: Treatment period 1: Tmax of total radioactivity in plasma following administration of IV dose of [14C]-GSK3640254 Time: Screening, Day-1, Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate GSK3640254 in plasma.
Measure: Treatment period 2: Tmax in plasma following administration of oral dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate total radioactivity in plasma.
Measure: Treatment period 2: Tmax of total radioactivity in plasma following administration of oral dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate total radioactivity in blood.
Measure: Treatment period 2: Tmax of total radioactivity in blood following administration of oral dose of [14C]-GSK3640254 Time: Day 1 (2, 4, 6, 8, 10 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate [14C]-GSK3640254 in plasma.
Measure: Treatment period 1:Terminal phase half-life (T1/2) in plasma following administration of IV dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate GSK3640254 in plasma.
Measure: Treatment period 1: T1/2 in plasma following administration of oral dose of GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate total radioactivity in plasma.
Measure: Treatment period 1: T1/2 of total radioactivity in plasma following administration of IV dose of [14C]-GSK3640254 Time: Screening, Day-1, Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate GSK3640254 in plasma.
Measure: Treatment period 2: T1/2 in plasma following administration of oral dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points to evaluate total radioactivity in plasma.
Measure: Treatment period 2: T1/2 of total radioactivity in plasma following administration of oral dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points for pharmacokinetic analysis of [14C]-GSK3640254.
Measure: Treatment period 1: Volume of distribution at steady state (Vss) following administration of IV dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points for pharmacokinetic analysis of [14C]-GSK3640254.
Measure: Treatment period 1: Total systemic clearance (CL) following administration of IV dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Urine samples will be collected at the indicated time points for pharmacokinetic analysis of GSK3640254.
Measure: Treatment period 1: Renal clearance (CLr) following administration of IV dose of GSK3640254 Time: Day 1 (Pre-dose), 0-24 Hours, 24-48 Hours, 48-72 Hours, 72-96 Hours, 96-120 Hours, 120-144 Hours, 144-168 HoursDescription: Urine samples will be collected at the indicated time points for pharmacokinetic analysis of GSK3640254.
Measure: Treatment period 2: CLr following administration of oral dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose), 0-24 Hours, 24-48 Hours, 48-72 Hours, 72-96 Hours, 96-120 Hours, 120-144 Hours, 144-168 HoursDescription: Blood samples will be collected at the indicated time points for pharmacokinetic analysis of GSK3640254.
Measure: Treatment period 1: Oral Clearance (CL/F) following oral dose of GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points for pharmacokinetic analysis of GSK3640254.
Measure: Treatment period 2: CL/F following oral dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points for pharmacokinetic analysis of GSK3640254.
Measure: Treatment period 1: Apparent volume of distribution (Vz/F) following oral dose of GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points for pharmacokinetic analysis of GSK3640254.
Measure: Treatment period 2: Vz/F following oral dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points for pharmacokinetic analysis of GSK3640254.
Measure: Treatment period 1: Absolute oral bioavailability (F) of GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points for pharmacokinetic analysis of GSK3640254.
Measure: Treatment period 1: Percentage of drug escaping first pass hepatic clearance (Fh) following administration of GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8,9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points for pharmacokinetic analysis of GSK3640254.
Measure: Treatment period 1: Percentage of drug absorbed (Fa) following administration of GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Blood samples will be collected at the indicated time points for pharmacokinetic analysis of GSK3640254.
Measure: Treatment period 1: Percentage of drug escaping gut metabolism (Fg) following administration of GSK3640254 Time: Day 1 (Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 4.5, 5, 5.25, 6, 7, 8, 9, 10, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose)Description: Urine samples will be collected at the indicated time points to determine total radioactivity in urine.
Measure: Treatment period 1: Percentage of total radioactive dose in urine following administration of IV dose of [14C]-GSK3640254 Time: Day 1 (Pre-dose), 0-24 Hours, 24-48 Hours, 48-72 Hours 72 - 96 Hours, 96-120 Hours, 120-144 Hours, 144-168 HoursDescription: Urine samples will be collected at the indicated time points to determine total radioactivity in urine.
Measure: Treatment period 2: Percentage of the total radioactive dose in urine following administration of oral dose of [14C]-GSK3640254 Time: 0-24 Hours, 24-48 Hours, 48-72 Hours, 72-96 Hours, 96-120 Hours, 120-144 Hours, 144-168 HoursDescription: Fecal samples will be collected at the indicated time points to determine total radioactivity in feces.
Measure: Treatment period 1: Percentage of total radioactive dose in feces following administration of IV dose of [14C]-GSK3640254 Time: 0-24 Hours, 24-48 Hours, 48- 72 Hours, 72-96 Hours, 96-120 Hours, 120-144 Hours, 144-168 Hours.Description: Fecal samples will be collected at the indicated time points to determine total radioactivity in feces.
Measure: Treatment period 2: Percentage of total radioactive dose in feces following administration of oral dose of [14C]-GSK3640254 Time: 0-24 Hours, 24-48 Hours, 48-72 Hours, 72-96 Hours, 96-120 Hours, 120-144 Hours, 144-168 Hours.Description: AEs and SAEs will be collected.
Measure: Number of participants With Adverse Events (AEs) and Serious AEs (SAEs) Time: Up to 50 daysDescription: Blood samples and urine samples will be collected for assessment of hematology, clinical chemistry and urine parameters.
Measure: Number of participants with abnormal hematology, clinical chemistry and urinalysis parameters Time: Day -1, Day 2 (36 hours), Day 5 , Day 8 and up to 50 daysDescription: Single12-lead ECG will be recorded with the participant in a supine position. Number of participants with abnormal ECG findings will be assessed.
Measure: Number of participants with abnormal 12-lead electrocardiogram (ECG) Time: Up to 50 daysDescription: Number of participants with abnormal vital signs will be assessed.
Measure: Number of participants with abnormal vital signs Time: Up to 50 daysDescription: Blood samples will be collected at the indicated time points to evaluate total radioactivity following administration of oral dose of [14C]-GSK3640254.
Measure: Treatment Period 2: Total radioactivity in blood to plasma following administration of oral dose of [14C]-GSK3640254 Time: 2 Hours, 4 Hours, 6 Hours, 8 Hours, and 10 Hours