to Evaluate the Safety, Tolerability and Pharmacokinetics of Four Formulations of LY03009 in Healthy Volunteers

An Open-Label Study in Healthy Volunteers to Evaluate the Safety, Tolerability and Pharmacokinetics of Four Formulations of LY03009 After a Single Intramuscular Injection

The purpose of this study is to Evaluate the Safety, Tolerability and Pharmacokinetics of Four Formulations of LY03009 in Healthy Volunteers.

Study Overview

• Status: Enrolling by invitation
• Conditions: Parkinson's Disease
• Intervention / Treatment: Drug: LY03009 F1; Drug: LY03009 F2; Drug: LY03009 F3; Drug: LY03009 F4

Detailed Description

This is an open-label study in healthy volunteers to evaluate the safety, tolerability and pharmacokinetics of four formulations of LY03009 (F1, F2, F3, F4) after a single intramuscular injection.

Approximately 40 healthy subjects are planned to be enrolled in this study and assigned to four cohorts (F1, F2, F3, F4) sequentially, 10 subjects per group at a fixed dose of 112 mg for F1~F3 and 224 mg for F4. Each subject will receive only one dose in this study.

• Study Type: Interventional
• Enrollment (Anticipated): 40
• Phase: Phase 1

Contacts and Locations

Study Locations

• Australia
  • South Australia
    • Adelaide, South Australia, Australia, 5000
      • CMAX Clinical Research Pty Ltd

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 65 years (ADULT, OLDER_ADULT)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria：

To participate in the study, subjects must meet all of the following inclusion criteria:

1. Willing and capable of giving signed written informed consent;
2. Male or female, 18-65 years of age (inclusive) at screening;
3. Body mass index (BMI, weight [kg]/height [m]2) between 18.0 and 30.0 kg/m2, inclusive;
4. The screening results within the normal range or outside the normal range but assessed as clinically non-significant by the Investigator based on detailed medical history, clinical laboratory tests, vital signs, physical examination, and 12-lead ECG; QTcF ≤450 msec for male subjects, and QTcF ≤470 msec for female subjects.
5. Males who are willing to remain abstinent; or if engaging in sexual intercourse with a female partner of childbearing potential, willing to use a condom in addition to having the female partner use a highly effective method of contraception throughout the study and until at least 3 months after the end of the study. This requirement does not apply to subjects in a same sex relationship or subjects with female partners of non-childbearing potential. Male subjects must also be willing to not donate sperm throughout the study and until at least 3 months after the end of the study.

Exclusion Criteria：

Subjects meeting any of the following criteria will be excluded from the study:

1. With history of history of gastrointestinal, cardiovascular, musculoskeletal, endocrine, hematologic, psychiatric, renal, hepatic, neurologic, bronchopulmonary, immunologic, and/or lipid metabolism disorders, and/or drug hypersensitivity, or any other condition that, in the opinion of the PI, would jeopardize the safety of the subject, affect the validity of the study results, or impair the ability to provide informed consent;
2. Hospital admission or major surgery within 3 months prior to screening, or plan to have surgery before the completion of study;
3. Receipt of another investigational product within 1 month or 5 half-lives of the other investigational product, whichever is longer, before study drug administration in this study;
4. Unwillingness or inability to comply with food and beverage restrictions during study participation;
5. Have a history of significant drug sensitivity or drug allergy, or known hypersensitivity to the study drugs, the metabolite or formulation excipients;
6. Malignancy within 5 years of screening visit (excluding non-melanoma skin cancer and cervical carcinoma in situ that has been completely resected);
7. Subject who is considered unsuitable for participating in the study in the opinion of investigator.
8. Recent administration of live vaccine within 3 months prior to dosing and until at least 30 days after the completion of the study.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: TREATMENT
• Allocation: RANDOMIZED
• Interventional Model: SEQUENTIAL
• Masking: NONE

Number of Arms

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
EXPERIMENTAL: Formulation 1; a single dose of LY03009 F1	Drug: LY03009 F1; a single dose of LY03009 F1
EXPERIMENTAL: Formulation 2; a single dose of LY03009 F2	Drug: LY03009 F2; a single dose of LY03009 F2
EXPERIMENTAL: Formulation 3; a single dose of LY03009 F3	Drug: LY03009 F3; a single dose of LY03009 F3
EXPERIMENTAL: Formulation 4; a single dose of LY03009 F4	Drug: LY03009 F4; a single dose of LY03009 F4

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Frequency of adverse events	Frequency of adverse events. Apply to cohort F1, cohort F2 and cohort F3.	From screening up to day 98
Frequency of adverse events	Frequency of adverse events. Apply to cohort F4.	From screening up to day 161

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Maximum (peak) plasma concentration (Cmax) of LY03009	Maximum (peak) plasma concentration (Cmax) of LY03009. Apply to cohort F1, cohort F2 and cohort F3.	From screening up to day 98
Maximum (peak) plasma concentration (Cmax) of LY03009	Maximum (peak) plasma concentration (Cmax) of LY03009. Apply to cohort F4	From screening up to day 161
Area under the plasma concentration-time curve from time zero to the last measurable concentration (AUC0-t) of LY03009	Area under the plasma concentration-time curve from time zero to the last measurable concentration (AUC0-t) of LY03009.Apply to cohort F1, cohort F2 and cohort F3.	From screening up to day 98
Area under the plasma concentration-time curve from time zero to the last measurable concentration (AUC0-t) of LY03009	Area under the plasma concentration-time curve from time zero to the last measurable concentration (AUC0-t) of LY03009.Apply to cohort F4	From screening up to day 161
Area under the plasma concentration-time curve from time zero to infinity (AUC0-∞) of LY03009	Area under the plasma concentration-time curve from time zero to infinity (AUC0-∞) of LY03009.Apply to cohort F1, cohort F2 and cohort F3.	From screening up to day 98
Area under the plasma concentration-time curve from time zero to infinity (AUC0-∞) of LY03009	Area under the plasma concentration-time curve from time zero to infinity (AUC0-∞) of LY03009. Apply to cohort F4	From screening up to day 161
Time to maximum plasma concentration (Tmax) of LY03009	Time to maximum plasma concentration (Tmax) of LY03009. Apply to cohort F1, cohort F2 and cohort F3.	From screening up to day 98
Time to maximum plasma concentration (Tmax) of LY03009	Time to maximum plasma concentration (Tmax) of LY03009. Apply to cohort F4	From screening up to day 161
Terminal elimination half-life (t1/2) of LY03009	Terminal elimination half-life (t1/2) of LY03009. Apply to cohort F1, cohort F2 and cohort F3.	From screening up to day 98
Terminal elimination half-life (t1/2) of LY03009	Terminal elimination half-life (t1/2) of LY03009.Apply to cohort F4	From screening up to day 161
Apparent clearance (CL/F) of LY03009	Apparent clearance (CL/F) of LY03009. Apply to cohort F1, cohort F2 and cohort F3.	From screening up to day 98
Apparent clearance (CL/F) of LY03009	Apparent clearance (CL/F) of LY03009. Apply to cohort F4	From screening up to day 161
Apparent volume of distribution (Vz/F) of LY03009	Apparent volume of distribution (Vz/F) of LY03009. Apply to cohort F1, cohort F2 and cohort F3.	From screening up to day 98
Apparent volume of distribution (Vz/F) of LY03009	Apparent volume of distribution (Vz/F) of LY03009. Apply to cohort F4	From screening up to day 161
Terminal elimination rate constant (λz) of LY03009	Terminal elimination rate constant (λz) of LY03009. Apply to cohort F1, cohort F2 and cohort F3.	From screening up to day 98
Terminal elimination rate constant (λz) of LY03009	Terminal elimination rate constant (λz) of LY03009. Apply to cohort F4	From screening up to day 161
Mean residence time (MRT) of LY03009	Mean residence time (MRT) of LY03009. Apply to cohort F1, cohort F2 and cohort F3.	From screening up to day 98
Mean residence time (MRT) of LY03009	Mean residence time (MRT) of LY03009. Apply to cohort F4	From screening up to day 161
Area under the plasma concentration-time curve extrapolated from time t to infinity as a percentage of total AUC (%AUCex) of LY03009	Area under the plasma concentration-time curve extrapolated from time t to infinity as a percentage of total AUC (%AUCex) of LY03009. Apply to cohort F1, cohort F2 and cohort F3.	From screening up to day 98
Area under the plasma concentration-time curve extrapolated from time t to infinity as a percentage of total AUC (%AUCex) of LY03009	Area under the plasma concentration-time curve extrapolated from time t to infinity as a percentage of total AUC (%AUCex) of LY03009. Apply to cohort F4	From screening up to day 161

Collaborators and Investigators

• Sponsor: Luye Pharma Group Ltd.
• Investigators: Principal Investigator: Angela Molga, CMAX Clinical Research Pty Ltd

Study record dates

Study Major Dates

• Study Start (ACTUAL): February 2, 2021
• Primary Completion (ANTICIPATED): October 1, 2021
• Study Completion (ANTICIPATED): October 1, 2021

Study Registration Dates

• First Submitted: September 21, 2020
• First Submitted That Met QC Criteria: October 13, 2020
• First Posted (ACTUAL): October 20, 2020

Study Record Updates

• Last Update Posted (ACTUAL): June 8, 2021
• Last Update Submitted That Met QC Criteria: June 3, 2021
• Last Verified: June 1, 2021

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Brain Diseases; Central Nervous System Diseases; Nervous System Diseases; Parkinsonian Disorders; Basal Ganglia Diseases; Movement Disorders; Synucleinopathies; Neurodegenerative Diseases; Parkinson Disease
• Other Study ID Numbers: LY03009/CT-AUS-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