The Study of a Selective 5-ht6 Receptor Antagonist, HEC30654AcOH,in Healthy Subjects

Safety, Tolerability, and Pharmacokinetics Phase ⅠStudy of a Selective 5-ht6 Receptor Antagonist, HEC30654AcOH, Following Single and Multiple Ascending Doses，Single-center, Randomized, Double-blind in Healthy Subjects

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.

Study Overview

• Status: Unknown
• Conditions: Healthy
• Intervention / Treatment: Drug: HEC30654AcOH capsule; Drug: Placebo capsule

Detailed Description

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.

• Study Type: Interventional
• Enrollment (Anticipated): 99
• Phase: Phase 1

Contacts and Locations

Study Locations

• China
  • Jilin
    • Changchun, Jilin, China, 130000
      • First Hospital of Jilin University

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 45 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• signing informed consent, and fully understanding the study's content, process，possible adverse reaction before the study beginning.
• Be able to complete the study in accordance with the requirements of the study.
• Subjects (including partner) which from screening to the last time of study drug dosage volunteered to take effective contraceptive measures within 6 months, see appendix for birth control measures.
• Age of 18 to 45 years old male and female subjects (including 18 and 45 years of age).
• Male subjects not less than 50 kg, female subjects not less than 45 kg weight.Body mass index (BMI) = weight (kg)/height 2 (m2), body mass index (BMI) within the scope of 18 ~ 28 kg/m2 (including threshold).
• Physical examination, vital signs is normal or abnormal has no clinical significance.

Exclusion Criteria:

• 3 months before the study daily smoking more than 5 pieces.
• having allergies or allergic constitution for experiment drugs (a variety of drugs and food allergies).
• Has a history of drug and/or binge drinking (drinking 14 units of alcohol every week: 1 unit = 285 mL beer, or liquor 25 mL, or wine 100 mL).
• Three months before screening blood or blood loss (> 450 mL).
• 28 days before the screening taking any drugs of changing liver enzymes.
• Within 14 days before the screening taken any prescription drugs, over-the-counter drugs, vitamins or herbal products.
• Within 2 weeks before the screening taking any special diet (including dragon fruit, mango, pomelo, etc.) or with vigorous exercise, or other affect drug absorption, distribution, metabolism and excretion.
• With the following CYP3A4, P - gp or Bcrp inhibitors or inducers, such as itraconazole, ketone health zun or definitely nida, lung, etc.
• Recently, very large changes in diet or exercise habits.
• Three months before taking study drug, there taken study drug and its analogues, or participated in drug clinical trials.
• Having difficulty swallowing or any digestive system diseases history affecting drug absorption, excretion,etc.
• Having had any increased risk of hemorrhagic disease, such as hemorrhoids, acute gastritis or gastric and duodenal ulcer, etc.
• Abnormal ecg that have clinical significance.
• Female subjects in screening test is in lactation or have positive serum pregnancy outcomes.
• Clinical laboratory examination were abnormal clinical significance, or other clinical findings show that there are clinical significance of the following diseases (including but not limited to the gastrointestinal tract, liver, kidney, and nerve, blood, endocrine, tumor, lung, immune, spirit, or disease of heart head blood-vessel).
• Viral hepatitis (including hepatitis b and c),, treponema pallidum antibody , HIV antibody positive.
• From the screening stage to study medicine had a acute disease or taken a drugs.
• Within 48 hours before taking the study drug, there taken any caffeine consumed chocolate, or rich xanthine food or drinks.
• Within 24 hours before taking study drug, there used any alcoholic products or alcohol-breath test was positive.
• Urine drug test(Morphine and marijuana) was positive.
• Neurological examination had abnormal findings, and researchers think have clinical significance.
• Researchers think that doesn't fit to the study.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Parallel Assignment
• Masking: Quadruple

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: HEC30654AcOH capsule; 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.	Drug: HEC30654AcOH capsule; 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.
Placebo Comparator: placebo capsule; 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.	Drug: Placebo capsule; 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.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	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

Secondary Outcome Measures

Outcome Measure	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)	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

Collaborators and Investigators

• Sponsor: Sunshine Lake Pharma Co., Ltd.

Study record dates

Study Major Dates

• Study Start (Actual): November 21, 2018
• Primary Completion (Anticipated): October 30, 2019
• Study Completion (Anticipated): November 30, 2019

Study Registration Dates

• First Submitted: August 24, 2018
• First Submitted That Met QC Criteria: August 30, 2018
• First Posted (Actual): August 31, 2018

Study Record Updates

• Last Update Posted (Actual): April 4, 2019
• Last Update Submitted That Met QC Criteria: April 2, 2019
• Last Verified: April 1, 2019

More Information

Terms related to this study

• Other Study ID Numbers: HEC30654-P-01

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: No

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No