A Study Assessing the Safety and Tolerability of LY03020 in Chinese Healthy Subjects

A Phase Ⅰ, Randomized, Double-blind, Placebo-controlled, Single Dose Ascending Study to Assess the Safety, Tolerability, and Pharmacokinetics of LPM787000048 Maleate Sustained-release Tablet (LY03020) in Chinese Healthy Adult Subjects

This is a single-center, randomized, double-blind, placebo-controlled, ascending single oral dose study to assess the safety, tolerability, and pharmacokinetics of LY03020 in Chinese healthy adult subjects.

Study Overview

• Status: Completed
• Conditions: Schizophrenia; Alzheimer's Disease Psychosis
• Intervention / Treatment: Drug: LY03020; Drug: Placebo

Detailed Description

The study will set 2.5mg, 5mg, 10mg, 20mg, 40mg, 60mg, 80mg and 100mg, a total of 8 dose groups. Qualified subjects were enrolled in site at D-1 ( 1 day before administration ) and randomized.The subjects should fast for at least 10 hours before medication administration, with no restrictions on water intake. The subjects will be required to orally take LY03020 or a placebo on an empty stomach upon waking on D1 (the day of medication administration). From D1 to D7, they will undergo safety assessments and PK biological sample collection.

• Study Type: Interventional
• Enrollment (Actual): 66
• Phase: Phase 1

Contacts and Locations

Study Locations

• China
  • Beijing, China
    • Beijing Anding Hospital Capital Medical University

Participation Criteria

Eligibility Criteria

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

Description

Inclusion Criteria:

• Subjects sign informed consent voluntarily.
• Male or female aged 18 to 45 years.
• Body weight ≥ 50.0 kg for male and ≥ 45.0 kg for female, and male or female greater than or equal to 18.5 but less than 26.0 kg/m2 of body mass index (BMI).

Exclusion Criteria:

• Subjects have any clinically significant medical condition or chronic disease.
• Subjects experienced a history of keratopathy, fundus disease, increased intraocular pressure,or angle-closure glaucoma.Subjects have a abnormal and clinically significant test for ophthalmic examination during screening.
• Subjects with condition that may interfere with the drug absorption, distribution, metabolism and excretion significantly.
• Subjects had a history of surgery within 3 months prior to administration, or had not recovered, or have a surgical plan during the study.
• Subjects have any clinically significant abnormal vital signs, laboratory values, and ECGs.
• Subjects have used any of nonprescription drugs within 7 days or prescription drugs within 28 days prior to administration.
• Subjects have a history of allergic diseases, or allergic to any substance contained in the formulation
• Subjects have a positive test for HBsAg, HCV-Ab, HIV-Ab, or syphilis serum reaction.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Parallel Assignment
• Masking: Triple

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: LY03020; Subjects will take single-dose LY03020 on Day 1	Drug: LY03020; LY03020 for one single dose; Other Names: LPM787000048 Maleate sustained-release tablet
Sham Comparator: Placebo; Subjects will take single-dose Placebo on Day 1	Drug: Placebo; Placebo for one single dose; Other Names: Placebo of LPM787000048 Maleate sustained-release tablet

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Frequency of adverse events (AEs)	Percentage of adverse events	up to144 hours

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Maximum observed concentration (Cmax) of LPM787000048 in plasma	Subject blood samples will be collected at 17 time points and pharmacokinetic parameters will be calculated.	up to144 hours
Time to maximum observed concentration (Tmax) of LPM787000048 in plasma	Subject blood samples will be collected at 17 time points and pharmacokinetic parameters will be calculated.	up to144 hours
Area under the concentration-time curve from time zero extrapolated to infinity (AUC0-∞) of LPM787000048 in plasma	Subject blood samples will be collected at 17 time points and pharmacokinetic parameters will be calculated.	up to144 hours
Area under the concentration-time curve from time zero to the time of last quantifiable concentration (AUC0-t) of LPM787000048 in plasma	Subject blood samples will be collected at 17 time points and pharmacokinetic parameters will be calculated.	up to144 hours
Apparent terminal elimination half-life (t1/2) of LPM787000048 in plasma	Subject blood samples will be collected at 17 time points and pharmacokinetic parameters will be calculated.	up to144 hours
Apparent volume of distribution（Vz/F） of LPM787000048 in plasma	Subject blood samples will be collected at 17 time points and pharmacokinetic parameters will be calculated.	up to144 hours
Apparent total body clearance (CL/F) of LPM787000048 from plasma	Subject blood samples will be collected at 17 time points and pharmacokinetic parameters will be calculated.	up to144 hours

Other Outcome Measures

Outcome Measure	Measure Description	Time Frame
Quantitatively determine the concentration of LPM787000048 and major metabolites (if applicable) in urine and calculate the cumulative excretion ratio in urine.	One dose group will be selected for metabolite identification.	up to144 hours

Collaborators and Investigators

• Sponsor: Luye Pharma Group Ltd.
• Investigators: Principal Investigator: Gang Wang, Beijing Anding Hospital Capital Medical University

Study record dates

Study Major Dates

• Study Start (Actual): August 19, 2024
• Primary Completion (Actual): February 13, 2025
• Study Completion (Actual): February 13, 2025

Study Registration Dates

• First Submitted: August 13, 2024
• First Submitted That Met QC Criteria: August 13, 2024
• First Posted (Actual): August 16, 2024

Study Record Updates

• Last Update Posted (Actual): May 29, 2025
• Last Update Submitted That Met QC Criteria: May 23, 2025
• Last Verified: May 1, 2025

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Brain Diseases; Central Nervous System Diseases; Nervous System Diseases; Schizophrenia Spectrum and Other Psychotic Disorders; Mental Disorders; Neurocognitive Disorders; Dementia; Tauopathies; Neurodegenerative Diseases; Schizophrenia; Alzheimer Disease; Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Maleic acid
• Other Study ID Numbers: LY03020/CT-CHN-101

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
• product manufactured in and exported from the U.S.: No