This open-label, randomized, 4-way crossover study in healthy participants will determine the relative bioavailability of the tablet formulation relative to the capsule formulation and the effect of a high-fat and low-fat meal on the relative bioavailability of the tablet formulation.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Three 90 milligram \[mg\] capsules of GDC-0276 administered orally.
Three 90 mg GDC-0276 tablets administered orally.
Quotient Clinical Ltd, Clinical Research Unit
Nottingham, United Kingdom
Relative Bioavailability: Geometric Mean Ratio (Tablet/Capsule) of Log Transformed Cmax of M12 Metabolite of GDC-0276
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Relative Bioavailability: Geometric Mean Ratio (Tablet/Capsule) of Log Transformed Maximum Plasma Concentration (Cmax) of GDC-0276
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Relative Bioavailability: Geometric Mean Ratio (Tablet/Capsule) of Log Transformed Cmax of M16 Metabolite of GDC-0276
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Relative Bioavailability: Geometric Mean Ratio (Tablet/Capsule) of Log Transformed Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of GDC-0276
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Relative Bioavailability: Geometric Mean Ratio (Tablet/Capsule) of Log Transformed Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClastu) of M12 Metabolite of GDC-0276
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Relative Bioavailability: Geometric Mean Ratio (Tablet/Capsule) of Log Transformed Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClastu) of M16 Metabolite of GDC-0276
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
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Relative Bioavailability: Geometric Mean Ratio (Tablet/Capsule) of Log Transformed Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - inf)] of GDC-0276
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Relative Bioavailability: Geometric Mean Ratio (Tablet/Capsule) of Log Transformed Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - inf)] of M12 Metabolite of GDC-0276
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Relative Bioavailability: Geometric Mean Ratio (Tablet/Capsule) of Log Transformed Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - inf)] of M16 Metabolite of GDC-0276
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Time to Reach Maximum Observed Plasma Concentration (Tmax) of GDC-0276 Following High-fat Meals, low-fat Meals and in Fasted State on a Tablet Dosing
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Time to Reach Maximum Observed Plasma Concentration (Tmax) of M12 Metabolite of GDC-0276 Following High-fat Meals, low-fat Meals and in Fasted State on a Tablet Dosing
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Time to Reach Maximum Observed Plasma Concentration (Tmax) of M16 Metabolite of GDC-0276 Following High-fat Meals, low-fat Meals and in Fasted State on a Tablet Dosing
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Apparent Oral Clearance (CL/F) of GDC-0276 Following Tablet and Capsule Dosing
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Apparent Oral Clearance (CL/F) of M12 Metabolite of GDC-0276 Following Tablet and Capsule Dosing
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Apparent Oral Clearance (CL/F) of M16 Metabolite of GDC-0276 Following Tablet and Capsule Dosing
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Apparent Volume of Distribution (Vz/F) of GDC-0276 Following Tablet and Capsule Dosing
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Apparent Volume of Distribution (Vz/F) of M12 Metabolite of GDC-0276 Following Tablet and Capsule Dosing
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Plasma Terminal Half-Life (t1/2) of GDC-0276 Following High-fat Meals, low-fat Meals and in Fasted State on a Tablet Dosing
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Plasma Terminal Half-Life (t1/2) of M12 Metabolite of GDC-0276 Following High-fat Meals, low-fat Meals and in Fasted State on a Tablet Dosing
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Plasma Terminal Half-Life (t1/2) of M16 Metabolite of GDC-0276 Following High-fat Meals, low-fat Meals and in Fasted State on a Tablet Dosing
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose
Number of Participants With Adverse Events and Serious Adverse Event
Time frame: Baseline up to Follow up (Day 32)
Apparent Volume of Distribution (Vz/F) of M16 Metabolite of GDC-0276 Following Tablet and Capsule Dosing
Time frame: Pre-dose (within 0.5 hours of dosing), 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 48, 72, 96, 120, 144 hours post-Day 1, or Day 7, or Day 13, or Day 19 dose