Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
GS-4571 · 1 trial · 1 indication
AUCinf is defined as area under the concentration versus time curve extrapolated to infinite time.
Cmax is defined as the maximum observed concentration of drug in plasma.
AUCtau is defined as area under the concentration versus time curve over the dosing interval.
Cmax is defined as the maximum observed concentration of drug in plasma.
| Arm | Type | Description |
|---|---|---|
| Part A Single-ascending Dose (SAD) in Healthy Participants | EXPERIMENTAL | Participants will be randomized into 4 + (optional) 1 dose escalating cohorts and will receive GS-4571 or placebo to match (PTM) GS-4571 on Day 1, to determine the maximum tolerated dose: * Cohort 1: Dose 1 GS-4571, administered orally as a single dose, in a fasting state. * Cohort 2: Dose 2 GS-4571, administered orally as a single dose, in a fasting state. * Cohort 3: Dose 3 GS-4571, administered orally as a single dose, in a fasting state. * Cohort 4: Dose 4 GS-4571, administered orally as a single dose, in a fasting state. * Cohort 5 (optional): Dose 5 GS-4571, administered orally as a single dose, in a fasting state. |
| Part B Food/PPI Effect in Healthy Participants | EXPERIMENTAL | Participants will be randomized into 2 sequence groups in Cohort 6 and will receive the highest dose found to be safe and well tolerated in Part A of GS-4571 and omeprazole. The two sequential groups will receive the following treatments: * Treatment A: Up to the highest single dose of GS-4571 evaluated in Part A, fasting. * Treatment B: Up to the highest single dose of GS-4571 evaluated in Part A, nonfasting (high-fat/high-calorie meal). * Treatment C (optional): Omeprazole, once-daily (QD) for 5 days, fasting. * Treatment D (optional): Omeprazole followed by up to the highest single dose of GS-4571 evaluated in Part A, 2 hours later, fasting. |
| Part C Multiple-ascending Dose (MAD) in Nondiabetic Obese Participants | EXPERIMENTAL | Participants randomized in Cohorts 7-9 will be randomized to receive up to 4 escalating doses of GS-4571 or PTM QD for 12 weeks, as follows: * Cohort 7: Up to dose determined from Part A of GS-4571 or PTM in obese participants, QD, in a non-fasting state * Cohort 8: Up to 3-fold the Cohort 7 dose of GS-4571 or PTM in obese participants, QD, in a non-fasting state * Cohort 9: Up to 2-fold the Cohort 8 dose of GS-4571 or PTM in obese participants, QD, in a non-fasting state * Cohort 10 is optional and will receive GS-4571 or PTM QD for 12 weeks in case it is opened for enrollment as follows: * Up to 2-fold the Cohort 9 dose of GS-4571 or PTM in obese participants, QD, in a non-fasting state. |
| Part D Multiple Dose in Nonobese Participants With T2DM | EXPERIMENTAL | Participants randomized in Cohort 11 will receive up to the highest dose of GS-4571 or PTM in T2DM, QD, in a non-fasting state for 12 weeks. |
| Name | Type | Description |
|---|---|---|
| GS-4571 | DRUG | Administered orally |
| Placebo | DRUG | Administered orally |
| Omeprazole | DRUG | Administered orally |
Key Inclusion Criteria: * Individuals must be glucagon-like peptide-1 receptor agonist (GLP-1RA) naïve OR last dose was at least 6 months prior to screening. * Part A (SAD) and Part B (Food/PPI Effect): eligible individuals in Cohorts 1-4, (optional cohort 5) and 6 will include healthy individuals ...