A Study to Assess Serotonin Transporter Occupancy of Healthy Adults Using 11C-DASB PET

A Non-Randomized, Open-Label, Exploratory Mechanistic Validation (PoM) Clinical Trial of LV232 Capsule Assessing Serotonin Transporter Occupancy in the Healthy Adult Brain Using 11C-DASB Positron Emission Tomography (PET)

This study was a non-randomized, open-label clinical study to assess Serotonin transporter occupancy in the brain of healthy adults using 11C-DASB positron emission tomography (PET)

Study Overview

• Status: Completed
• Conditions: Major Depressive Disorder
• Intervention / Treatment: Drug: LV232 40mg; Drug: Escitalopram 20 mg; Drug: LV232 60mg; Drug: LV232 20mg

Detailed Description

This trial adopts a single-center, non-randomized, open-label design, with a planned enrollment of 16 healthy subjects. The LV232 capsule groups include 6 subjects in the 40 mg dose group, 4 subjects in the 60 mg dose group, and 4 subjects in the 20 mg dose group. Additionally, there are 2 subjects in the escitalopram oxalate tablet (positive control drug) group. Based on the results of the LV232 capsule study, the investigator and sponsor will jointly decide whether to proceed with the positive control group, using escitalopram oxalate tablets at a dose of 20 mg as the positive control drug.

• Study Type: Interventional
• Enrollment (Actual): 20
• Phase: Phase 1

Contacts and Locations

Study Locations

• China
  • Shanghai, China
    • Shanghai Mental Health Center Ethics Committee

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: Adult
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• Those who voluntarily participate in and sign the informed consent form after understanding the purpose, content, process and possible risks of the trial;
• Male and female, aged 18 to 45 years at the time of signing the informed consent form;
• Body weight, male≥ 50.0 kg ,female≥ 45.0 kg ,and body mass index (BMI) 19.0 ~ 26.0 kg/m2 (including the boundary value) at screening;
• Able to maintain good communication with the investigator and comply with the lifestyle restrictions specified in the protocol and various requirements of the clinical trial (scheduled visits, laboratory tests and other trial procedures);
• Subjects and their partners must use effective non-pharmacological contraception (e.g., abstinence and condom with intravaginal spermicide) throughout the study and for 6 months after the end of the study, and must not donate sperm.

Exclusion Criteria:

• Known to have a history of allergy to any component of the investigational product or similar drugs, or allergic constitution (previous allergy to two or more foods or drugs);
• The subject with skin diseases or has a history of skin allergies;
• The subject has a current or past medical history judged by the investigator that may affect the clinical trial or dysfunction, including but not limited to a past or present central nervous system, cardiovascular system, digestive system, respiratory system, urinary system, blood system, metabolic disorders, etc. that require medical intervention or other diseases that are not suitable for clinical trials (such as a history of mental illness);
• Individuals with a history of epileptic seizures, or those with any (acute or chronic) history of mental illness and family history of mental illness, or those with a history of neurodegenerative diseases and family history of neurodegenerative diseases, such as Alzheimer's disease;
• Any surgical condition or condition that may significantly affect the absorption, distribution, metabolism and excretion of the drug, or may pose a hazard to the subjects participating in the trial; such as history of gastrointestinal surgery (gastrectomy, gastrointestinal anastomosis, intestinal resection, etc.), urinary tract obstruction or dysuria, gastroenteritis, gastrointestinal ulcers, gastrointestinal bleeding, etc.;
• Abnormal vital signs (resting pulse rate<55 beats/minute or>100 beats/minute; Systolic blood pressure<90 mmHg or ≥ 140 mmHg; Diastolic blood pressure<60 mmHg or ≥ 90 mmHg), laboratory tests (blood routine , blood biochemistry, urine routine, thyroid Function), 12 electrocardiogram (ECG, male QTcF>450 ms，female QTcF>460 ms), MRI (magnetic resonance imaging) examination indicators, judged by the investigator as abnormal and clinically significant;
• Use of any prescription medication within 28 days prior to dosing; Use of any over-the-counter medications, including health products, within 7 days prior to dosing; Receipt of any contrast agent or radiopharmaceutical within 7 days prior to, or application of contrast agent within 24 hours after, administration of the trial drug;
• Contraindications to PET or MRI (magnetic resonance imaging) (including claustrophobia, alcohol allergy, cardiac pacemaker and nerve stimulator in the body, metal foreign body in the body or tracer component allergy, etc.);
• Any positive result of hepatitis B surface antigen (HBsAg), hepatitis C antibody (HCV-Ab), HIV antibody (HIV-Ab) and Toluidine red unheated serum test (Trust);
• Smoking habit (an average daily smoking of ≥ 5 cigarettes per day within 3 months before administration), drinking habit (an average weekly drinking of more than 14 standard units within 3 months before administration, 1 unit = 360 mL of beer or 45 mL of 40% spirits or 150 mL of wine). Subjects who cannot quit smoking or drinking in clinical trials.
• Individuals who have a history of drug dependence (including drug use) within one year prior to administration, or who have tested positive for urinary drug abuse screening (benzodiazepines, cocaine, methamphetamine, amphetamine, methadone, tetrahydrocannabinol acid, barbiturates, morphine, phencyclidine, tricyclic antidepressants);
• Those who have special requirements for food and cannot abide by the unified diet or have dysphagia;
• Consumption of xanthine-rich foods or beverages (e.g., tea, coffee, cola, or chocolate) or foods or beverages containing grapefruit and/or pomelo within 3 days before dosing;
• Significant occupational exposure to ionizing radiation (e.g., more than 50 millivolts per year) or exposure to radioactive substances or ionizing radiation for therapeutic or research purposes within the past year;
• Blood donation or blood loss ≥ 400 mL within 3 months before administration, or blood donation or blood loss ≥ 200 mL within one month;
• Those who have participated in other clinical trials within 3 months before administration (including drug and medical device clinical trials, the time is based on the last visit, except for those who have failed screening in other clinical trials and have not received any treatment);
• Pregnant, lactating women or male subjects whose spouses have a parenting plan within 3 months;
• Individuals who cannot tolerate intravenous administration ;
• Personnel directly related to this clinical trial;
• Patients with poor compliance or other problems who are not suitable for participating in this trial in the opinion of the investigator.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Non-Randomized
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Active Comparator: Escitalopram; A single oral dose of 20mg Escitalopram (10 mg/tablet, 2 tablets each time) , administrated with 240 mL water	Drug: Escitalopram 20 mg; oral; Other Names: Escitalopram
Experimental: LV232; A single oral dose of 40mg LV232 (5 mg/capsule, 8 capsules each time) ，administrated in fasting state, with 240 mL water to take A single oral dose of 60mg LV232 (5 mg/capsule, 12 capsules each time) ，administrated in fasting state, with 240 mL water to take A single oral dose of 20mg LV232 (5 mg/capsule, 4 capsules each time) ，administrated in fasting state, with 240 mL water to take	Drug: LV232 40mg; oral; Other Names: LV232; Drug: LV232 60mg; oral; Other Names: LV232; Drug: LV232 20mg; oral; Other Names: LV232

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Serotonin Transporters occupancy	Percentage of Serotonin Transporters Occupancy in Human Brain after oral LV232 capsule	baseline and 3 hours after administration on Day 1

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Incidence of treatment-emergent adverse events (TEAEs).	Incidence of treatment-emergent adverse events (TEAEs)	Up to Day 7

Collaborators and Investigators

• Sponsor: Vigonvita Life Sciences
• Investigators: Principal Investigator: Yifeng SHEN, MD, Shanghai Mental Health Center

Study record dates

Study Major Dates

• Study Start (Actual): May 30, 2024
• Primary Completion (Actual): January 19, 2025
• Study Completion (Actual): May 23, 2025

Study Registration Dates

• First Submitted: June 18, 2024
• First Submitted That Met QC Criteria: June 24, 2024
• First Posted (Actual): June 26, 2024

Study Record Updates

• Last Update Posted (Actual): June 10, 2025
• Last Update Submitted That Met QC Criteria: June 8, 2025
• Last Verified: February 1, 2025

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Mental Disorders; Mood Disorders; Depressive Disorder; Depressive Disorder, Major; Physiological Effects of Drugs; Molecular Mechanisms of Pharmacological Action; Autonomic Agents; Peripheral Nervous System Agents; Neurotransmitter Agents; Membrane Transport Modulators; Psychotropic Drugs; Neurotransmitter Uptake Inhibitors; Antiparkinson Agents; Anti-Dyskinesia Agents; Antidepressive Agents; Serotonin Agents; Selective Serotonin Reuptake Inhibitors; Antidepressive Agents, Second-Generation; Muscarinic Antagonists; Cholinergic Antagonists; Cholinergic Agents; Parasympatholytics; Escitalopram; Citalopram; Dexetimide
• Other Study ID Numbers: LV232-03

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