PK/PD Study of YZJ-1139

NCT06685341 | Completed Phase 1

• 1 other identifier: YZJ-1139-1-02
• Study Type: interventional
• Target: 20
• Locations: 1 country
• Sites: 1

Brief Summary

Primary Objective： To determine the dose-response relationship of YZJ-1139 in young and elderly Chinese subjects after a single oral administration of different doses, and to compare it with zolpidem at clinical doses. Secondary Objective: To investigate the safety and tolerability of YZJ-1139 in young and elderly Chinese subjects after a single oral administration of different doses, and to compare it with zolpidem at clinical doses.

Conditions

Insomnia

Outcome Measures

Primary Outcomes (24)

• Cmax of YZJ-1139、zolpidem

  Cmax is defined as the maximum concentration of drug

  From Day 1 to Day 2 post single dose；up to 4 weeks

• AUCinf of YZJ-1139、zolpidem

  AUCinf is defined as the concentration of drug extrapolated to infinite time

  From Day 1 to Day 2 post single dose；up to 4 weeks

• AUClast of YZJ-1139、zolpidem

  AUClast is defined as the concentration of drug from time zero to the last observable concentration

  From Day 1 to Day 2 post single dose；up to 4 weeks

• Tmax of YZJ-1139、zolpidem

  Tmax is defined as the time (observed time point) of Cmax

  From Day 1 to Day 2 post single dose；up to 4 weeks

• t1/2 of YZJ-1139、zolpidem

  From Day 1 to Day 2 post single dose；up to 4 weeks

• CL/F of YZJ-1139、zolpidem

  CL/F is defined as the apparent oral clearance following administration of the drug

  From Day 1 to Day 2 post single dose；up to 4 weeks

• Vz/F of YZJ-1139、zolpidem

  Vz/F is defined as the apparent volume of distribution of the drug

  From Day 1 to Day 2 post single dose；up to 4 weeks

• Left and right saccade peak velocity (SPV) of Eye Movements

  Instruct the subject to fix their gaze on the red light spot on the LED display and move their eyes with the light spot. During the test, the head and body must remain still. The test consists of the following two parts, each lasting 2 minutes. Between the two parts, the subject should rest for a certain period of time based on their level of fatigue. Part 1: Scanning eye movements Part 2: Smooth pursuit eye movements.

  From Day 1 to Day 2 post single dose；up to 4 weeks

• left and right saccade accuracy rate (SacAcc) of Eye Movements

  Instruct the subject to fix their gaze on the red light spot on the LED display and move their eyes with the light spot. During the test, the head and body must remain still. The test consists of the following two parts, each lasting 2 minutes. Between the two parts, the subject should rest for a certain period of time based on their level of fatigue. Part 1: Scanning eye movements Part 2: Smooth pursuit eye movements.

  From Day 1 to Day 2 post single dose；up to 4 weeks

• Left and right saccade eye movement response time (SacRT) of Eye Movements

  Instruct the subject to fix their gaze on the red light spot on the LED display and move their eyes with the light spot. During the test, the head and body must remain still. The test consists of the following two parts, each lasting 2 minutes. Between the two parts, the subject should rest for a certain period of time based on their level of fatigue. Part 1: Scanning eye movements Part 2: Smooth pursuit eye movements.

  From Day 1 to Day 2 post single dose；up to 4 weeks

• Smooth eye movement to the left and right (Smooth) of Eye Movements

  Instruct the subject to fix their gaze on the red light spot on the LED display and move their eyes with the light spot. During the test, the head and body must remain still. The test consists of the following two parts, each lasting 2 minutes. Between the two parts, the subject should rest for a certain period of time based on their level of fatigue. Part 1: Scanning eye movements Part 2: Smooth pursuit eye movements.

  From Day 1 to Day 2 post single dose；up to 4 weeks

• Body Sway

  The subject takes off their shoes, spreads their feet shoulder-width apart, and stands on a flat ground 120 cm away from the measuring device. They close their eyes and stand for 2 minutes, and the test measures the body sway amplitude (mm) of the subject during the 2-minute closed-eye period. The test evaluates the subject's postural balance

  From Day 1 to Day 2 post single dose；up to 4 weeks

• Simple response time of Choice Reaction Time Test

  The test lasts for 1 minute. During the test, there is a vertical line in the center of the screen. On both sides of the screen, random "left" or "right" words will appear. The participants are required to ignore the word meanings and click the "right" or "left" key based on the word's position.

  From Day 1 to Day 2 post single dose；up to 4 weeks

• Simple response accuracy rate of Choice Reaction Time Test

  The test lasts for 1 minute. During the test, there is a vertical line in the center of the screen. On both sides of the screen, random "left" or "right" words will appear. The participants are required to ignore the word meanings and click the "right" or "left" key based on the word's position.

  From Day 1 to Day 2 post single dose；up to 4 weeks

• Selective response time of Choice Reaction Time Test

  During the test, there was a dividing line in the middle of the screen. During the test, the word "left" or "right" appeared randomly on both sides of the screen. Subjects were asked to ignore the position of the word and click the key "right" or "left" according to the meaning of the word.

  From Day 1 to Day 2 post single dose；up to 4 weeks

• Selective response accuracy rate of Choice Reaction Time Test

  During the test, there was a dividing line in the middle of the screen. During the test, the word "left" or "right" appeared randomly on both sides of the screen. Subjects were asked to ignore the position of the word and click the key "right" or "left" according to the meaning of the word.

  From Day 1 to Day 2 post single dose；up to 4 weeks

• The average reaction time for correct responses of Digit Symbol Substitution Test

  The test time is not more than 2 minutes, the symbol is displayed on the screen, and the subject clicks the corresponding number according to the corresponding relationship between the symbol and the number given below. After clicking or exceeding the upper limit of the reaction time, the subject automatically enters the next symbol.

  From Day 1 to Day 2 post single dose；up to 4 weeks

• The number of correct responses of Digit Symbol Substitution Test

  The test time is not more than 2 minutes, the symbol is displayed on the screen, and the subject clicks the corresponding number according to the corresponding relationship between the symbol and the number given below. After clicking or exceeding the upper limit of the reaction time, the subject automatically enters the next symbol.

  From Day 1 to Day 2 post single dose；up to 4 weeks

• The average reaction time for incorrect responses of Digit Symbol Substitution Test

  The test time is not more than 2 minutes, the symbol is displayed on the screen, and the subject clicks the corresponding number according to the corresponding relationship between the symbol and the number given below. After clicking or exceeding the upper limit of the reaction time, the subject automatically enters the next symbol.

  From Day 1 to Day 2 post single dose；up to 4 weeks

• The number of incorrect responses of Digit Symbol Substitution Test

  The test time is not more than 2 minutes, the symbol is displayed on the screen, and the subject clicks the corresponding number according to the corresponding relationship between the symbol and the number given below. After clicking or exceeding the upper limit of the reaction time, the subject automatically enters the next symbol.

  From Day 1 to Day 2 post single dose；up to 4 weeks

• The number of non-responses of Digit Symbol Substitution Test

  The test time is not more than 2 minutes, the symbol is displayed on the screen, and the subject clicks the corresponding number according to the corresponding relationship between the symbol and the number given below. After clicking or exceeding the upper limit of the reaction time, the subject automatically enters the next symbol.

  From Day 1 to Day 2 post single dose；up to 4 weeks

• Immediate recall of Word Recall Test

  About 1-2 hours after dosing， First, the subjects were shown 20 unrelated words, each word for a few seconds, and then the subjects were asked to immediately recall the words they just saw. The number of correct words in instantaneous recall was recorded respectively

  From Day 1 to Day 2 post single dose；up to 4 weeks

• Delayed recall of Word Recall Test

  About 1-2 hours later, the subjects were allowed to freely recall the words again, which was delayed recall; The number of correct words in delayed recall was recorded respectively

  From Day 1 to Day 2 post single dose；up to 4 weeks

• Delayed recognition of Word Recall Test

  The subjects were then presented with 40 words (of which 20 were previously presented words and 20 were confounding words), and were asked to answer one by one whether they were the words they had just seen. The number of correct words in delayed extraction was recorded respectively

  From Day 1 to Day 2 post single dose；up to 4 weeks

Secondary Outcomes (1)

• Adverse events (AEs)

  From Day 1 to Day 2 post single dose；up to 4 weeks

Study Arms (4)

Drug: YZJ-1139 high dose group

EXPERIMENTAL

Subjects will be into two groups：Young adult subjects and elderly subjects

Drug: YZJ-1139

Drug: YZJ-1139 low dose group

EXPERIMENTAL

Subjects will be into two groups：Young adult subjects and elderly subjects

Drug: YZJ-1139

Drug: Placebo

PLACEBO COMPARATOR

Drug: Placebo

Drug: Zolpidem

ACTIVE COMPARATOR

Drug: Zolpidem

Interventions

YZJ-1139 DRUG

YZJ-1139

Drug: YZJ-1139 high dose group; Drug: YZJ-1139 low dose group

Placebo DRUG

Oral tablet

Drug: Placebo

Zolpidem DRUG

Oral tablet

Drug: Zolpidem

Eligibility Criteria

• Age: 18 Years - 75 Years
• Sex: all
• Healthy Volunteers: No
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Young adults and elderly Chinese healthy subjects, both male and female;
• Age: \[young adult group\] 18-45 years old (including the threshold value); \[Elderly group\]65\~75 years old (including the cut-off value);
• Body weight \[only for young adults\]: ≥50kg, BMI: 18\~28kg/m2 (including the threshold value);
• Understand and sign the informed consent to participate in the study.

You may not qualify if:

• History of heart, liver, lung, kidney, digestive tract, blood system, neuropsychiatric system and other diseases, including anxiety and depression, that researchers deem clinically significant;
• Comprehensive physical examination, neurological examination, laboratory examination, ECG examination, etc. indicate that the subject has abnormalities that are judged by the researcher as clinically significant;
• Poor compliance with the pharmacodynamics training before administration;
• Have taken any medication in the two weeks prior to study administration, and the investigator judges it may affect the evaluation results;
• History of food and drug allergy or allergic reaction that the researcher determines to be clinically significant;
• Serological examination (HBsAg, anti-HCV, anti-HIV, TP-Ab) with positive results;
• History of alcohol or drug abuse within the year prior to study administration that the investigators believe may have affected the results assessed in this study;
• Frequent (\> 1 time per month) use of hypnotic drugs, and screening and baseline benzodiazepine urine screening positive;
• Participants who need to work night shifts, stay up late, or stay at least 3 time zones away from the study site within 2 weeks before and during the study;
• Subjects who could not maintain a regular sleep and rest schedule (get up at 6-8 am and go to sleep at 10-12 PM) within 1 week before and during the study and who were judged by the investigator to be likely to affect the results of this study;
• Those who could not quit smoking and alcohol drinking as required during the study period or whose carbon monoxide breath test detected \>7 ppm during the screening period (further confirmation by urine cotinine test if deemed necessary by the investigators);
• Participants who have participated in any drug clinical trial as a subject within 3 months prior to study administration;
• Patients who donated blood or blood products ≥400 mL or 2 units within three months prior to drug administration;
• Those who do not agree to avoid the use of tobacco, alcohol or caffeinated beverages, or to avoid strenuous exercise, or to avoid other factors affecting the absorption, distribution, metabolism or excretion of drugs within 24 hours before and during the trial;
• Don't agree or is unable to refrain from eating grapefruit or other related tropical fruits and beverages and from using St. John's Wort during the 24 hours prior to the first dose and during the study period;

Sponsors & Collaborators

• Shanghai Haiyan Pharmaceutical Technology Co., Ltd.: lead

Study Sites (1)

Beijing Tiantan Hospital, Capital Medical University

Beijing, China

Location

MeSH Terms

Conditions

Sleep Initiation and Maintenance Disorders

Interventions

Zolpidem

Condition Hierarchy (Ancestors)

Sleep Disorders, Intrinsic; Dyssomnias; Sleep Wake Disorders; Nervous System Diseases; Mental Disorders

Intervention Hierarchy (Ancestors)

Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: DOUBLE
• Who Masked: PARTICIPANT, INVESTIGATOR
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: Single dose, four-cycle crossover

Study Record Dates

• First Submitted: November 7, 2024
• First Posted: November 12, 2024
• Study Start: March 7, 2019
• Primary Completion: April 10, 2019
• Study Completion: November 15, 2019
• Last Updated: November 12, 2024

Record last verified: 2024-11

Locations

CN (1)