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This 4-part study will assess the effect of formulation, food, and active pharmaceutical ingredient (API) lot on the pharmacokinetics of GDC-0032 in healthy volunteers. Part 1 is an open-label, 3-period, 6-sequence study, and Parts 2, 3, and 4 are open-label 2-period crossover studies. Participants will receive single doses of GDC-0032 capsule or tablet formulation, in the fasted or fed state.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Part 1: Food Effect | Experimental | GDC-0032 will be administered orally over 3-Treatment Period (TP) in 6-sequence as one 3 milligrams (mg) capsule in TP-A after 10 hour fasting from food, one 3 mg Phase III tablet in TP-B after 10 hour fasting from food and one 3 mg Phase III tablet in TP-C following the start of standard Food and Drug Administration (FDA) high-fat breakfast. Washout period o 14 to 20 days will be given between each TP. |
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| Part 2: Tablet Formulation Comparison | Experimental | Different formulations of tablets (Tablet A and Tablet B) of GDC-0032 will be administered orally over 2-TP having 10 hour fasting from food. Participants will receive one 3 mg Tablet A in TP-A and one 3 mg Tablet B in TP-B after 14 to 20 days washout period. |
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| Part 3: Capsule API Lot Comparison | Experimental | Two different lots of GDC-0032 active pharmaceutical ingredient (API) capsule formulation will be administered orally in crossover fashion over 2-TP to 20 participants having 10 hour fasting from food. Participants will receive one 3 mg capsule in TP-A and one 3 mg capsule in TP-B after 14 to 20 days washout period. |
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| Part 4: Tablet Relative Bioavailibity | Experimental | GDC-0032 will be administered orally in crossover fashion over 2-TP to 20 participants having 10 hour fasting from food. Participants will receive one 3 mg capsule in TP-A and one 2 mg Phase III tablet in TP-B after 14 to 20 days washout period. |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| GDC-0032 Phase III Tablet | Drug | Participants will receive 2 mg or 3 mg Phase III tablet after 10 hour fasting from food. |
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| Measure | Description | Time Frame |
|---|---|---|
| Area Under the Concentration-Time Curve From Hour 0 to the Last Measurable Concentration (AUC0-t) | Pre-dose (Hour 0), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 168, 192 hour post-dose | |
| Area Under the Concentration-Time Curve Extrapolated to Infinity (AUC0-infinity) | Pre-dose (Hour 0), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 168, 192 hour post-dose | |
| Maximum Plasma Concentration (Cmax) | Pre-dose (Hour 0), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 168, 192 hour postdose |
| Measure | Description | Time Frame |
|---|---|---|
| Time to Maximum Plasma Concentration (tmax) | Pre-dose (Hour 0), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 168, 192 hour post-dose | |
| Apparent Terminal Elimination Rate Constant | Pre-dose (Hour 0), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 168, 192 hour post-dose |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Clinical Trials | Genentech, Inc. | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Covance Research Unit - Dallas | Dallas | Texas | 75247 | United States |
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| GDC-0032 Tablet | Drug | Participants will receive 3 mg Tablet A or Tablet B formulation after 10 hour fasting from food. |
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| GDC-0032 Capsule | Drug | Participants will receive 3 mg GDC-0032 capsule formulation after 10 hour fasting from food. |
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| Apparent Terminal Elimination Constant (t1/2) | Pre-dose (Hour 0), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 168, 192 hour post-dose |
| Apparent Total Clearance (CL/F) | Pre-dose (Hour 0), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 168, 192 hour post-dose |
| Apparent Volume of Distribution (Vz/F) | Pre-dose (Hour 0), 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, 168, 192 hour post-dose |
| Percentage of Participants With Adverse Events | From Baseline up to approximately 15 weeks |
| ID | Term |
|---|---|
| C582924 | 2-(3-(2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo(f)imidazo(1,2-d)(1,4)oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide |
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