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The study consists of 5 dose groups, starting at 25 mg, 6 subjects in 25 mg group, and 8 subjects in each other group (male or female), randomly assigned to study drug or placebo group to evaluate the safety, tolerability and PK characteristics. The subject number of single dose group may increase or decrease depending on the safety and PK data obtained. The dose levels are planned at 25 mg, 200 mg, 400 mg, 800 mg and 1200 mg. Based on observed tolerability and safety data or obtained PK data, adjustments are allowed at all dose levels in the clinical trial.
4 subjects in the 25 mg dose group will receive VV116 tablets and the other 2 subjects will receive placebo. In other dose groups, 6 subjects in each group will receive VV116 tablets and 2 subjects will receive placebo. 25mg,800mg and 1200 mg dose group will be given by sentinel administration (i.e. 1 study drug, 1 placebo). Subjects who receive sentinel administration will be observed for 48 hours and investigator will evaluate the safety parameters (including symptoms, vital signs, physical examination, etc.).
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| VV116 | Experimental | Subjects will receive VV116 orally for single dose. |
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| Placebo | Experimental | Subjects will receive placebo orally for single dose. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| VV116 25mg Group | Drug | 4 subjects will receive VV116 25mg,orally; 2 subjects will receive placebo,orally. |
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| Measure | Description | Time Frame |
|---|---|---|
| Incidence of Treatment-Emergent Adverse Events | Incidence of Treatment-Emergent Adverse Events | 7 days after treatment |
| Tmax | time at which Cmax occurs | From time zero up to 48 hours post-dose following oral administration of VV116 |
| Cmax | maximum observed plasma concentration | From time zero up to 48 hours post-dose following oral administration of VV116 |
| AUC0~t | area under the plasma concentration time curve from time zero to the last measurable concentration | From time zero up to 48 hours post-dose following oral administration of VV116 |
| AUC0-∞ | area under the plasma concentration-time curve from time zero to infinity | From time zero up to 48 hours post-dose following oral administration of VV116 |
| Measure | Description | Time Frame |
|---|---|---|
| structural of metabolites | Structure of main metabolites of VV116 in plasma, feces and urin. The main metabolites may include 116-N1 and M2. | From time zero up to 72 hours post-dose following oral administration of VV116 |
| Ae(total excretion of kidney) |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Gangyi Liu | Shanghai Xuhui Central Hospital | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Shanghai Xuhui Central Hospital | Shanghai | Shanghai Municipality | 200031 | China |
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| ID | Term |
|---|---|
| C000722705 | GS-621763 |
| D044382 | Population Groups |
| ID | Term |
|---|---|
| D003710 | Demography |
| D011154 | Population Characteristics |
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| VV116 200mg Group | Drug | 6 subjects will receive VV116 200mg,orally; 2 subjects will receive placebo,orally. |
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| VV116 400mg Group | Drug | 6 subjects will receive VV116 400mg,orally; 2 subjects will receive placebo,orally. |
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| VV116 800mg Group | Drug | 6 subjects will receive VV116 800mg,orally; 2 subjects will receive placebo,orally. |
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| VV116 1200mg Group | Drug | 6 subjects will receive VV116 1200mg,orally; 2 subjects will receive placebo,orally. |
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Ae(total excretion of kidney) |
| From time zero up to 72 hours post-dose following oral administration of VV116 |
| Ae%(proportion of excretion of kidney) | Ae%(proportion of excretion of kidney) | From time zero up to 72 hours post-dose following oral administration of VV116 |
| CLr(renal clearance rate) | CLr(renal clearance rate) | From time zero up to 72 hours post-dose following oral administration of VV116 |
| Cumulative excretion and percentage of VV116 and major metabolites in feces. | Cumulative excretion and percentage of VV116 and major metabolites in feces. | From time zero up to 72 hours post-dose following oral administration of VV116 |