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This study will characterize the pharmacokinetics (PK) of AK0529, the effect of food and evaluate the safety of AK0529 in healthy Chinese adult subjects. 50 subjects will be randomized to receive a dose level of AK0529 or placebo in five groups. The total study duration will be approximately 18-27 days for each subject.
This is a randomized, double-blind, placebo-controlled, single-center, Phase I study in healthy Chinese subjects. The objectives of the study are to evaluate the safety of AK0529, characterize the PK of AK0529 and to evaluate the effect of food in healthy Chinese subjects. 50 healthy Chinese subjects will be randomized to orally receive one of four dose levels of AK0529 (single dose:100 mg and 300 mg, Multiple dose: 600 mg, Cross-over Food Effect: 300 mg) or placebo. The total duration of the study will be approximately 18 to 27 days for each subject.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| AK0529 100 mg, Pilot | Experimental | This is an open pilot arm and male subjects enrolled into this arm will be only administered with an oral single dose of 100 mg AK0529. The dose group begins treatment on Day 1. |
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| AK0529 100 mg | Experimental | Subjects will be administered with an oral single dose of 100 mg AK0529 or placebo. The dose group begins treatment on Day 1. |
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| AK0529 300 mg, food effect | Experimental | A 3x3 cross-over study is designed in this group to evaluate the food effect following a standard Chinese meal or a high fat meal in the same subjects, comparing with the PK profile of AK0529 under fasted condition. Subjects will be administered with an oral dose of 300 mg AK0529 or placebo on Day 1 of each cycle. |
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| AK0529 600 mg | Experimental | Subjects will be administered with an oral single dose of 600 mg AK0529 or placebo. The dose group begins treatment on Day 1. |
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| AK0529 300 mg, MAD | Experimental | Subjects will be administered with the multiple doses of 300 mg AK0529 or placebo on Day 1-7. |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| AK0529 | Drug | Active Substance: AK0529, Pharmaceutical Form: Capsule, Route of Administration: Oral |
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| Measure | Description | Time Frame |
|---|---|---|
| Maximum Observed Plasma Concentration (Cmax) | The maximum observed plasma concentration of AK0529. | Day1 (pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12 hrs post-dose), Day2 (24 hrs post-dose), Day3 (48 hrs post-dose), Day4 (72 hrs post-dose), Day5, Day6, Day7, Day8, Day9 and Day10 |
| Time to Maximum Plasma Concentration (Tmax) | The time of occurrence of Cmax. | Day1 (pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12 hrs post-dose), Day2 (24 hrs post-dose), Day3 (48 hrs post-dose), Day4 (72 hrs post-dose), Day5, Day6, Day7, Day8, Day9 and Day10 |
| Area under the plasma concentration-time curve from time zero up to time (AUC 0-t) | The area under the plasma concentration-time curve from time zero up to the last analytically quantifiable concentration of AK0529. | Day1 (pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12 hrs post-dose), Day2 (24 hrs post-dose), Day3 (48 hrs post-dose), Day4 (72 hrs post-dose), Day5, Day6, Day7, Day8, Day9 and Day10 |
| Terminal Half-Life (t1/2) | The apparent elimination half-life of AK0529. | Day1 (pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12 hrs post-dose), Day2 (24 hrs post-dose), Day3 (48 hrs post-dose), Day4 (72 hrs post-dose), Day5, Day6, Day7, Day8, Day9 and Day10 |
| Area Under the Plasma Concentration-Time Curve Extrapolated to Infinity (AUC0-inf) | The area under the plasma concentration-time curve from time zero up extrapolated to infinity of AK0529. | Day1 (pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12 hrs post-dose), Day2 (24 hrs post-dose), Day3 (48 hrs post-dose), Day4 (72 hrs post-dose), Day5, Day6, Day7, Day8, Day9 and Day10 |
| Apparent Oral Clearance (CL/F) |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Jimmy Gu | info@arkbiosciences.com | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Shanghai Xuhui Central Hospital | Shanghai | 201203 | China |
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| ID | Term |
|---|---|
| C000707852 | ziresovir |
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| Placebo | Other | For assessment of the Adverse Event (AE) profile, there are placebo controls in each dose group (except the pilot group). The placebo is administered at the same time (and of the same dosage) as the AK0529 subjects. |
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| Placebo | Other | Active Substance: Placebo, Pharmaceutical Form: Capsule, Route of Administration: Oral |
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The oral clearance of AK0529 |
| Day1 (pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12 hrs post-dose), Day2 (24 hrs post-dose), Day3 (48 hrs post-dose), Day4 (72 hrs post-dose), Day5, Day6, Day7, Day8, Day9 and Day10 |
| Percentage of Subjects with Adverse Events (AEs) | An adverse event can be any unfavorable and unintended sign (including an abnormal laboratory finding, for example), symptom, or disease temporally associated with the use of a pharmaceutical product, whether or not considered related to the pharmaceutical product. | From baseline up to approximately 6 weeks |