The purpose of this study is to compare the safety, tolerability, pharmacokinetic (PK), and comparative bioavailability of repeated administration of GSBR-1290 in healthy overweight/obese participants.
This is a 2-part study in which Part 1 will compare the PK of GSBR-1290, administered as tablet and capsule, using a 2-period, 2-sequence, crossover design in approximately 16 healthy overweight/obese participants. Part 2 will evaluate multiple-ascending doses of GSBR-1290 tablet in 3 cohorts, using 3 different titration regimens. Secondly in Part 2, the study will evaluate the comparative bioavailability of GSBR-1290 tablet versus capsule at a potentially clinically efficacious dose at steady state in Cohort 3.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
QUADRUPLE
Enrollment
70
ERG Clinical (Clinical Pharmacology of Miami - CPMI)
Miami, Florida, United States
Syneos Miami Site
Miami, Florida, United States
Parexel Baltimore Early Phase Clinical Unit
Baltimore, Maryland, United States
Part 1: Analysis of Maximum Observed Plasma Concentration (Cmax) for GSBR-1290 at Specified Timepoints Pre-dose and Post-dose to Calculate Pharmacokinetic (PK) Parameters
Time frame: From start of study drug up to Day 10
Part 1: Analysis of Time to Maximum Observed Plasma Concentration (Tmax) for GSBR-1290 at Specified Timepoints Pre-dose and Post-dose to Calculate PK Parameters
Time frame: From start of study drug up to Day 10
Part 1: Analysis of Area Under the Plasma Concentration-time Curve From Time Zero to Last Quantifiable Concentration (AUC0-t) for GSBR-1290 at Specified Timepoints Pre-dose and Post-dose to Calculate PK Parameters
Time frame: From start of study drug up to Day 10
Part 1: Analysis of Area Under the Plasma Concentration-time Curve From 0 to infinity (AUC0-inf) for GSBR-1290 at Specified Timepoints Pre-dose and Post-dose to Calculate PK Parameters
Time frame: From start of study drug up to Day 10
Part 1: Analysis of Apparent Terminal Elimination Half-life (t1/2) for GSBR-1290 at Specified Timepoints Pre-dose and Post-dose to Calculate PK Parameters
Time frame: From start of study drug up to Day 10
Part 1: Analysis of Total Apparent Body Clearance (CL/F) for GSBR-1290 at Specified Timepoints Pre-dose and Post-dose to Calculate PK Parameters
Time frame: From start of study drug up to Day 10
Part 1: Analysis of Apparent Volume of Distribution (Vz/F) for GSBR-1290 at Specified Timepoints Pre-dose and Post-dose to Calculate PK Parameters
Time frame: From start of study drug up to Day 10
Part 2: Number of Participants With Adverse Events (AEs) and Serious AEs
Time frame: From start of study drug up to End of study (EOS) in Part 2 (up to Day 98)
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
Participants will receive matching-placebo oral capsules or tablets.
Part 2: Number of Participants With Severity of AEs
Time frame: From start of study drug up to EOS in Part 2 (up to Day 98)
Part 2: Number of Participants With Clinically Significant Change From Baseline in Vital Signs
Time frame: From start of study drug up to EOS in Part 2 (up to Day 98)
Part 2: Number of Participants With Clinically Significant Change From Baseline in Electrocardiogram (ECG) Parameters
Time frame: From start of study drug up to EOS in Part 2 (up to Day 98)
Part 2: Number of Participants With Clinically Significant Change From Baseline in Laboratory Parameters
Time frame: From start of study drug up to EOS in Part 2 (up to Day 98)
Part 1: Number of Participants With Adverse Events (AEs) and Serious AEs
Time frame: From start of study drug up to EOS in Part 1 (Day 17)
Part 1: Number of Participants Based on Severity of AEs
Time frame: From start of study drug up to EOS in Part 1 (Day 17)
Part 1: Number of Participants With Clinically Significant Change From Baseline in Vital Signs
Time frame: Baseline up to EOS in Part 1 (Day 17)
Part 1: Number of Participants With Clinically Significant Change From Baseline in Electrocardiogram (ECG) Parameters
Time frame: Baseline up to EOS in Part 1 (Day 17)
Part 1: Number of Participants With Clinically Significant Change From Baseline in Laboratory Parameters
Time frame: Baseline up to EOS in Part 1 (Day 17)
Part 2: Analysis of Maximum Observed Plasma Concentration (Cmax) for GSBR-1290 at Specified Timepoints Pre-dose and Post-dose to Calculate Pharmacokinetic (PK) Parameters
Time frame: From start of study drug up to Day 84
Part 2: Analysis of Time to Maximum Observed Plasma Concentration (Tmax) for GSBR-1290 at Specified Timepoints Pre-dose and Post-dose to Calculate PK Parameters
Time frame: From start of study drug up to Day 84
Part 2: Analysis of Area Under the Plasma Concentration-time Curve From Time Zero to the End of the Dosing Interval (24 hours) at Steady State (AUC0-tau) for GSBR-1290 at Specified Timepoints Pre-dose and Post-dose to Calculate PK Parameters
Time frame: From start of study drug up to Day 84
Part 2: Analysis of Plasma Trough Concentrations for GSBR-1290 at Specified Timepoints Pre-dose and Post-dose to Calculate PK Parameters
Time frame: From start of study drug up to Day 84
Part 2: Analysis of Apparent Terminal Elimination Half-life (t1/2) for GSBR-1290 at Specified Timepoints Pre-dose and Post-dose to Calculate PK Parameters
Time frame: From start of study drug up to Day 84