Healthy Volunteers
Conditions
Brief summary
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.
Detailed description
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.
Interventions
DRUGGSBR-1290 (Capsule/Tablet)
Participants will receive GSBR-1290 oral capsules or tablets.
DRUGGSBR-1290
Participants will receive GSBR-1290 oral tablets.
DRUGPlacebo
Participants will receive matching-placebo oral tablets.
DRUGPlacebo (Capsule/Tablet)
Participants will receive matching-placebo oral capsules or tablets.
Sponsors
Gasherbrum Bio, Inc., a wholly owned subsidiary of Structure Therapeutics
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
QUADRUPLE (Subject, Caregiver, Investigator, Outcomes Assessor)
Masking description
Part 1 is open-label, 2-period, 2-sequence, cross-over and Part 2 is double blinded
Eligibility
Sex/Gender
ALL
Age
18 Years to 75 Years
Healthy volunteers
Yes
Inclusion criteria
1. Provided evidence of a signed informed consent before any study-related activities are initiated and be willing to comply with all study procedures. 2. Healthy overweight or obese adult men and women. 3. Age greater then or equal to (\>=)18 and less than or equal to (\<=) 75 years. 4. Body mass index (BMI) \>=27.0 kilogram per square meter (kg/m\^2).
Exclusion criteria
1\. History or presence of clinically significant cardiovascular, pulmonary, hepatic, renal, hematological, gastrointestinal, endocrine, immunologic, dermatologic, or neurological disease.
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Part 2: Number of Participants With Clinically Significant Change From Baseline in Laboratory Parameters | From start of study drug up to EOS in Part 2 (up to Day 98) |
| 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 | 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 | 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 | 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 | 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 | 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 | From start of study drug up to Day 10 |
| Part 2: Number of Participants With Adverse Events (AEs) and Serious AEs | From start of study drug up to End of study (EOS) in Part 2 (up to Day 98) |
| Part 2: Number of Participants With Severity of AEs | 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 | 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 | From start of study drug up to EOS in Part 2 (up to Day 98) |
| 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 | From start of study drug up to Day 10 |
Secondary
| Measure | Time frame |
|---|---|
| Part 1: Number of Participants Based on Severity of AEs | 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 | Baseline up to EOS in Part 1 (Day 17) |
| Part 1: Number of Participants With Clinically Significant Change From Baseline in Electrocardiogram (ECG) Parameters | Baseline up to EOS in Part 1 (Day 17) |
| Part 1: Number of Participants With Clinically Significant Change From Baseline in Laboratory Parameters | 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 | 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 | 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 | 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 | 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 | From start of study drug up to Day 84 |
| Part 1: Number of Participants With Adverse Events (AEs) and Serious AEs | From start of study drug up to EOS in Part 1 (Day 17) |
Countries
United States
Outcome results
None listed