A Study of Multiple-ascending Doses of GSBR-1290 in Healthy Overweight/Obese Participants
Phase 1
Active, not recruiting
- Conditions
- Healthy Volunteers
- Interventions
- Registration Number
- NCT06139055
- Lead Sponsor
- Gasherbrum Bio, Inc
- 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.
Recruitment & Eligibility
- Status
- ACTIVE_NOT_RECRUITING
- Sex
- All
- Target Recruitment
- 70
Inclusion Criteria
- Provided evidence of a signed informed consent before any study-related activities are initiated and be willing to comply with all study procedures.
- Healthy overweight or obese adult men and women.
- Age greater then or equal to (>=)18 and less than or equal to (<=) 75 years.
- Body mass index (BMI) >=27.0 kilogram per square meter (kg/m^2).
Exclusion Criteria
- History or presence of clinically significant cardiovascular, pulmonary, hepatic, renal, hematological, gastrointestinal, endocrine, immunologic, dermatologic, or neurological disease.
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- CROSSOVER
- Arm && Interventions
Group Intervention Description Part 2 (Cohort 1): GSBR-1290/Placebo Tablet Placebo Participants will receive GSBR-1290 or matching-placebo oral tablets once daily for a total of 12 weeks. Part 2 (Cohort 2): GSBR-1290/Placebo Tablet Placebo Participants will receive GSBR-1290 or matching-placebo oral tablets once daily for a total of 12 weeks. Part 2 (Cohort 3): GSBR-1290/Placebo Tablet and GSBR-1290/Placebo Capsule GSBR-1290 (Capsule/Tablet) Participants will receive GSBR-1290 or matching-placebo oral tablets once daily for a total of 12 weeks. In the last 4 weeks, participants will be further randomized to GSBR-1290 capsules or tablets or matching-placebo at Week 9 to 10 followed by alternate (capsule or tablet) formulation of either GSBR-1290 or placebo at Week 11 to 12. Part 2 (Cohort 3): GSBR-1290/Placebo Tablet and GSBR-1290/Placebo Capsule Placebo (Capsule/Tablet) Participants will receive GSBR-1290 or matching-placebo oral tablets once daily for a total of 12 weeks. In the last 4 weeks, participants will be further randomized to GSBR-1290 capsules or tablets or matching-placebo at Week 9 to 10 followed by alternate (capsule or tablet) formulation of either GSBR-1290 or placebo at Week 11 to 12. Part 1 (Sequence 1: Capsule to Tablet): GSBR-1290 Capsule/GSBR-1290 Tablet GSBR-1290 (Capsule/Tablet) Participants will receive a single dose of GSBR-1290 oral capsule formulation on Day 1 in Treatment Period 1 followed by GSBR-1290 oral tablet formulation on Day 8 (Day 1 of Treatment Period 2). Part 1(Sequence 2: Tablet to Capsule): GSBR-1290 Tablet/GSBR-1290 Capsule GSBR-1290 (Capsule/Tablet) Participants will receive a single dose of GSBR-1290 oral tablet formulation on Day 1 in Treatment Period 1 followed by GSBR-1290 oral capsule formulation on Day 8 (Day 1 of Treatment Period 2). Part 2 (Cohort 1): GSBR-1290/Placebo Tablet GSBR-1290 Participants will receive GSBR-1290 or matching-placebo oral tablets once daily for a total of 12 weeks. Part 2 (Cohort 2): GSBR-1290/Placebo Tablet GSBR-1290 Participants will receive GSBR-1290 or matching-placebo oral tablets once daily for a total of 12 weeks.
- Primary Outcome Measures
Name Time Method 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 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 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 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 Laboratory Parameters From start of study drug up to EOS in Part 2 (up to Day 98)
- Secondary Outcome Measures
Name Time Method 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 1: Number of Participants With Clinically Significant Change From Baseline in Vital Signs Baseline up to EOS in Part 1 (Day 17) 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) 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 Electrocardiogram (ECG) Parameters Baseline up to EOS in Part 1 (Day 17) 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
Trial Locations
- Locations (3)
ERG Clinical (Clinical Pharmacology of Miami - CPMI)
šŗšøMiami, Florida, United States
Parexel Baltimore Early Phase Clinical Unit
šŗšøBaltimore, Maryland, United States
Syneos Miami Site
šŗšøMiami, Florida, United States