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This is a single-center, randomized, double-blind, placebo-controlled, first-in-human study in which the safety, tolerability, and pharmacokinetics of orally administered AP303 will be assessed in healthy adult subjects.
The study will consist of 2 parts: Part A is a single ascending doses (SAD) phase enrolling a total of 4 cohorts of healthy subjects; Part B is a multiple ascending doses (MAD) phase enrolling 3 cohorts of healthy subjects. One cohort of Part A will receive AP303 under both fasted and fed conditions to investigate the effect of food.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| AP303 | Experimental | AP303 |
|
| Placebo | Placebo Comparator | Placebo |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| AP303 50 μg | Drug | AP303 tablet |
| |
| AP303 150 μg |
| Measure | Description | Time Frame |
|---|---|---|
| Single Dose and Food Effect Safety Outcome Measures | Incidence and severity of adverse events (AEs), laboratory, ECG, and vital sign changes | From baseline to Day 14 (Day 29 for Food Effect) |
| Multiple Dose Safety Outcome Measures | Incidence and severity of AEs, laboratory, ECG, and vital sign changes. | From baseline to Day 28 |
| Cmax after single dose | PK characteristics after single dose | Pre-dose to 96 hours post-dose |
| Tmax after single dose | PK characteristics after single dose | Pre-dose to 96 hours post-dose |
| AUC0-last after single dose | PK characteristics after single dose | Pre-dose to 96 hours post-dose |
| AUC0-inf after single dose | PK characteristics after single dose | Pre-dose to 96 hours post-dose |
| t1/2 after single dose | PK characteristics after single dose | Pre-dose to 96 hours post-dose |
| CL/F after single dose | PK characteristics after single dose | Pre-dose to 96 hours post-dose |
| Measure | Description | Time Frame |
|---|---|---|
| Effect of Food on the single dose Cmax | Effect of food on the single dose PK | Pre-dose to 96 hours post-dose |
| Effect of Food on the single dose Tmax | Effect of food on the single dose PK |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Sam Francis, Doctor | Nucleus Network | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Nucleus Network Pty Ltd | Melbourne | Victoria | 3004 | Australia |
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| Drug |
AP303 tablet |
|
| AP303 300 μg | Drug | AP303 tablet |
|
| AP303 600 μg | Drug | AP303 tablet |
|
| Placebo 50 μg | Drug | Placebo tablet |
|
| Placebo 150 μg | Drug | Placebo tablet |
|
| Placebo 300 μg | Drug | Placebo tablet |
|
| Placebo 600 μg | Drug | Placebo tablet |
|
| Ae and CLR (if warranted) after single dose | PK characteristics after single dose | Pre-dose to 96 hours post-dose |
| V/F after single dose | PK characteristics after single dose | Pre-dose to 96 hours post-dose |
| Cmax after multiple dose | PK characteristics after multiple dose | Pre-dose to 12 hours post dose on Day 1; pre-dose to 96 hours post-dose on Day 14 |
| Tmax after multiple dose | PK characteristics after multiple dose | Pre-dose to 12 hours post dose on Day 1; pre-dose to 96 hours post-dose on Day 14 |
| AUC0-τ after multiple dose | PK characteristics after multiple dose | Pre-dose to 12 hours post dose on Day 1; pre-dose to 96 hours post-dose on Day 14 |
| Cav after multiple dose | PK characteristics after multiple dose | Pre-dose to 12 hours post dose on Day 1; pre-dose to 96 hours post-dose on Day 14 |
| t1/2 after multiple dose | PK characteristics after multiple dose | Pre-dose to 12 hours post dose on Day 1; pre-dose to 96 hours post-dose on Day 14 |
| Rac after multiple dose | PK characteristics after multiple dose | Pre-dose to 12 hours post dose on Day 1; pre-dose to 96 hours post-dose on Day 14 |
| Ae and CLR (if warranted) after multiple dose | PK characteristics after multiple dose | Pre-dose to 12 hours post dose on Day 1; pre-dose to 96 hours post-dose on Day 14 |
| V/F after multiple dose | PK characteristics after multiple dose | Pre-dose to 12 hours post dose on Day 1; pre-dose to 96 hours post-dose on Day 14 |
| Ctrough after multiple dose | PK characteristics after multiple dose | Pre-dose on Days 2, 3, 4, 5, 7, 12, and 13 |
| Pre-dose to 96 hours post-dose |
| Effect of Food on the single dose AUC0-last | Effect of food on the single dose PK | Pre-dose to 96 hours post-dose |
| Effect of Food on the single dose AUC0-inf | Effect of food on the single dose PK | Pre-dose to 96 hours post-dose |
| Effect of Food on the single dose t1/2 | Effect of food on the single dose PK | Pre-dose to 96 hours post-dose |
| Effect of Food on the single dose CL/F | Effect of food on the single dose PK | Pre-dose to 96 hours post-dose |
| Effect of Food on the single dose Ae and CLR (if warranted) | Effect of food on the single dose PK | Pre-dose to 96 hours post-dose |
| Effect of Food on the single dose V/F | Effect of food on the single dose PK | Pre-dose to 96 hours post-dose |