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This study is a safety, tolerability, and pharmacokinetics phase Ⅰstudy of a selective 5-ht6 receptor antagonist, HEC30654AcOH,in healthy subjects.This test is divided into two parts, the first part is the healthy adult subjects single ascending-dose research;The second part is the healthy adult subjects multiple ascending-dose research.
The single ascending-dose research:
There have set up seven dose group(5、10、15、30、60、90、120mg).The first group(5mg)contains 3 health subjects,Which have been a preliminary experimental group. Each other groups contains 10 health subjects(8 health subjects take experimental drugs,2 health subjects take the placebo).Within 15min before taking the medicine and after 0.5h, 1h, 1.5h, 2h, 4h, 6h, 8h, 10h, 12h, 24h, 48h, 72h, 96h, 120h to take blood samples for pharmacokinetics(PK) detection.
The multiple ascending-dose research:
There have set up three dose group(15、30、60mg).Each group contains 12 health subjects(10 health subjects take experimental drugs,2 health subjects take the placebo).Each dose group in D1-D7 8:00(±1h)in the morning, 18:00(±1h), with 240 ml warm water to take corresponding study drug,but Day 8 only 8:00(±1h) in the morning take subjects drugs.Total for 15 times.on the morning of day 1 within 15minutes before the first drug and after 0.5h, 1h, 1.5h, 2h, 4h, 6h, 8h, 10h, 12h, on the morning of Day 6, Day 7 and Day 8 within 15 minutes before the drug collecting blood sample test concentration, on the morning of Day8 medication after 0.5h 1h, 1.5h, 2h, 4h, 6h, 8h, 10h, 12h, 24h, 48h, 72h, 96h, 120h collects pharmacokinetics(PK) blood samples.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| HEC30654AcOH capsule | Experimental | single ascending-dose study: Including 7 dose groups(5-、10、15-、30-、60-、90-、120mg),Day1 ante meridiem(AM) 8:00 (±1h) with 240ml warm water to taking the experiment drug,On an empty stomach . multiple ascending-dose study: Including 3 dose groups(15-、30-、60mg),Day1-Day7 AM 8:00 (±1h), 18:00 Post Meridiem(PM) (±1h), with 240ml warm water to take the experiment drug On an empty stomach;Day8 AM 8:00 (±1h)with 240ml warm water to taking the experiment drug,On an empty stomach. |
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| placebo capsule | Placebo Comparator | single ascending-dose study: Including 6 dose groups(10、15-、30-、60-、90-、120mg),Day1 morning 8:00 (±1h) with 240ml warm water to taking the placebo capsule,On an empty stomach . multiple ascending-dose study: Including 3 dose groups(15-、30-、60mg),Day1-Day7 AM 8:00 (±1h), 18:00 PM (±1h), with 240ml warm water to take the placebo capsule on an empty stomach;Day8 AM 8:00 (±1h)with 240ml warm water to taking the placebo capsule,on an empty stomach. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| HEC30654AcOH capsule | Drug | single ascending-dose study: 5-、10-、15-、30-、60-、90-、120mg HEC30654AcOH capsule in day1. Multiple ascending-dose study: 15-、30-、60mgHEC30654AcOH capsule in day1-day7,2 times everyday. |
| Measure | Description | Time Frame |
|---|---|---|
| Adverse events of the single ascending-dose | To assess the safe and tolerability of the single ascending-dose | From the baseline to 6 days |
| Adverse events of the multiple ascending-dose | To assess the safe and tolerability of the multiple ascending-dose | From the baseline to 13 days |
| Measure | Description | Time Frame |
|---|---|---|
| Maximum Plasma Concentration(Cmax) | Maximum Plasma Concentration(Cmax)of HEC30654AcOH in single ascending-dose | Prior to dosing(0h)and 0.5h,1h,1.5h,2h,4h,6h,8h,10h,12h,24h,48h,72h,96h,120h after dosing |
| Area Under the Curve(AUC) |
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Inclusion Criteria:
Exclusion Criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| First Hospital of Jilin University | Changchun | Jilin | 130000 | China |
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| Placebo capsule | Drug | single ascending-dose study: 5-、10-、15-、30-、60-、90-、120mg placebo capsule in day1. Multiple ascending-dose study: 15-、30-、60mg placebo capsule in day1-day7,2 times everyday. |
|
Area Under the Curve(AUC) of HEC30654AcOH in single ascending-dose
| Prior to dosing(0h)and 0.5h,1h,1.5h,2h,4h,6h,8h,10h,12h,24h,48h,72h,96h,120h after dosing |
| Maximum Peak Time(Tmax) | Maximum Peak Time(Tmax) of HEC30654AcOH in single ascending-dose | Prior to dosing(0h)and 0.5h,1h,1.5h,2h,4h,6h,8h,10h,12h,24h,48h,72h,96h,120h after dosing |
| Mean Residence Time(MRT) | Mean Residence Time(MRT) of HEC30654AcOH in single ascending-dose | Prior to dosing(0h)and 0.5h,1h,1.5h,2h,4h,6h,8h,10h,12h,24h,48h,72h,96h,120h after dosing |
| Terminal elimination half-life(T1/2) | Terminal elimination half-life(T1/2) of HEC30654AcOH in single ascending-dose | Prior to dosing(0h)and 0.5h,1h,1.5h,2h,4h,6h,8h,10h,12h,24h,48h,72h,96h,120h after dosing |
| steady state plasma concentration(Css) | steady state plasma concentration(Css)of HEC30654AcOH in multiple ascending-dose | Prior to dosing(0h)and 0.5h,1h,1.5h,2h,4h,6h,8h,10h,12h after dosing day1,then Prior to dosing(0h)of day6,day7,day8,and 0.5h,1h,1.5h,2h,4h,6h,8h,10h,12h,24h,48h,72h,96h,120h after dosing day8 |