Tolerance, PK and PD Effects Study of TPN-672 in Chinese Healthy Volunteers
- Registration Number
- NCT03931668
- Lead Sponsor
- Shanghai Mental Health Center
- Brief Summary
This is a single-site, randomized, double-blind, placebo-controlled, incremental phase I clinical trial to evaluate preliminarily the tolerance, pharmacokinetics and pharmacodynamic effects of TPN672 maleate in Chinese healthy volunteers after single dose administration.
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- UNKNOWN
- Sex
- All
- Target Recruitment
- 62
- Body weight > 50kg(male) or > 45kg(female), 19 <BMI<26 kg/m2.
- Good communication with investigators, willingness and ability to abide by the lifestyle restrictions stipulated in clinical trial
- Women or men within childbearing age do not have a fertility plan within 3 months after the end of the trial, and agree to adopt contraceptive measures approved (such as intrauterine device, condom, sperm killing gel, condom, uterine cap, etc.) throughout the clinical trial period.
- Fully understand the purpose and requirements of the trial, voluntarily participate in the clinical trial and sign the written informed consent, can complete the entire trial process according to the requirements of the trial.
- Investigator determined that there were diseases or functional disorders affecting clinical trials, including, but not limited to, central nervous system, cardiovascular system, respiratory system, digestive system, urinary system, endocrine system and blood system.
- Mental illness or previous history of mental illness;
- Have a history of ophthalmic diseases, such as abnormal color vision, retinitis pigmentosa, macular degeneration, etc.
- Have a history of malignant tumors or other diseases that are not suitable for clinical trials;
- Any surgical condition or condition that may significantly affect drug absorption, distribution, metabolism and excretion, or that may pose a hazard to the subjects participating in the study, such as history of gastrointestinal surgery (gastrectomy, gastrointestinal anastomosis, intestinal resection, etc.), urinary tract obstruction or dysuria, gastroenteritis, gastrointestinal ulcer, gastrointestinal bleeding, etc.
- Those who are known to have a history of drug allergy, allergic disease or allergic constitution of the tested drug ingredients or similar drugs;
- Smokers who smoked more than 10 cigarettes or the same amount of tobacco per day in the first year of screening;
- Alcohol addiction within 1 year before screening, with an average weekly alcohol intake of more than 14 units (1 unit = 285 ml beer or 25 ml spirits or 150 ml wine) or positive alcohol breath test;
- Those who had a history of drug abuse or drug abuse within 1 year before screening, or those who had positive urinary drug screening;
- Physical examination, current medical history and vital signs were found to be abnormal by researchers and have clinical significance.
- Resting pulse rate < 55/min or > 100/min; systolic pressure < 90 mmHg or > 140 mmHg, diastolic pressure < 60 mmHg or > 90 mmHg;
- 12-lead electrocardiogram (ECG) examination was found to be abnormal by investigator and had clinical significance; or the following ECG abnormalities occurred: PR interval > 220 ms, QRS complex wave duration > 120 ms, long QT syndrome (QTc > 450 ms);
- Family history of sudden cardiac death (less than 40 years old);
- Abnormal blood routine examination and urine routine examination have clinical significance.
- Aspartate transferase (AST), alanine transferase (ALT), creatinine (Cr), urea nitrogen (BUN) exceeded the normal upper limit.
- HBsAg, HCV-Ab, HIV-Ab and TRUST positive patients;
- Pregnant or lactating women or male subjects whose spouses have child-rearing plans within three months;
- Those who took any medicine within 2 weeks before admission, including prescription and non-prescription drugs;
- Blood donation or blood loss (> 200 ml) within 3 months before admission, or a history of using blood products;
- Participated in any clinical trials within 3 months before admission;
- Those who had a history of operation within 3 months before admission, or who had not recovered from the operation, or who had anticipated operation plan during the trial period;
- Do not agree to abide by the following conditions during the experiment: prohibit the use of tobacco, alcohol or caffeine-containing beverages, avoid strenuous exercise;
- Personnel directly related to this clinical trial;
- Investigator believes that other subjects are not suitable for the study.
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- SEQUENTIAL
- Arm && Interventions
Group Intervention Description 0.125mg single dose TPN-672 single dose of TPN-672 0.125mg, 2 subjects 0.25mg single dose TPN-672 single dose of 0.25mg, 10 subjects (8 for TPN-672, 2 for placebo) 0.5mg single dose TPN-672 single dose of 0.5mg, 10 subjects (8 for TPN-672, 2 for placebo) 1mg single dose TPN-672 single dose of 1mg, 10 subjects (8 for TPN-672, 2 for placebo) 2mg single dose TPN-672 single dose of 2mg, 10 subjects (8 for TPN-672, 2 for placebo) 3mg single dose TPN-672 single dose of 3mg, 10 subjects (8 for TPN-672, 2 for placebo) 4mg single dose TPN-672 single dose of 4mg, 10 subjects (8 for TPN-672, 2 for placebo)
- Primary Outcome Measures
Name Time Method ACR 48 hours Apparent Clearance Rate
ADV 48 hours Apparent Distribution Volume
Cmax 48 hours Maximum Plasma Concentration
AUC 48 hours Area Under the Curve
Tmax 48 hours Time to Cmax
T1/2 48 hours Time of half life
Adverse events 48 hours Number of Subjects with adverse events during clinical trial
- Secondary Outcome Measures
Name Time Method prolactin 48 hours serum prolactin test
temperature 48 hours ear temperature
pulse rate 48 hours pulse rate
IL-1 48 hours Serum concentration of Interleukin-1
QTc 48 hours QTc interval
IL-2 48 hours Serum concentration of Interleukin-2
INF-gamma 48 hours Serum concentration of Interferon-gamma
TNF-alpha 48 hours Serum concentration of Tumor necrosis factor-alpha
5-HT 48 hours Serum concentration of serotonin
DA 48 hours Serum concentration of Dopamine
NE 48 hours Serum concentration of Norepinephrine
BDNF 48 hours Serum concentration of Brain-derived neurotrophic factor
Glutamic acid 48 hours Serum concentration of Glutamic acid
GABA 48 hours Serum concentration of gamma-aminobutyric acid
respiratory 48 hours frequency of respiratory per minute
blood pressure 48 hours lying blood pressureļ¼ systolic and diastolic
electrocardiogram(ECG) 48 hours the number of subjects with abnormal ECG report by 12-lead electrocardiogram
IL-4 48 hours Serum concentration of Interleukin-4
Extrapyramidal symptoms 48 hours Simpson Angus Rating Scale (SAS), total score ranges from 0 to 40, of which lower values represent a better outcome.
Involuntary Movement 48 hours Abnormal Involuntary Movement Scale (AIMS), total score ranges from 0 to 14, of which lower values represent a better outcome.
Akathisia 48 hours Barnes Akathisia Rating Scale (BARS), total score ranges from 0 to 40, of which lower values represent a better outcome.
IL-6 48 hours Serum concentration of Interleukin-6
Trial Locations
- Locations (1)
Shanghai Mental Health Center
šØš³Shanghai, Shanghai, China