Dose-Escalation Study to Assess the Safety, Tolerability, and Pharmacokinetics of Donepezil From Single Dose of GB-5001 IM Depot and Aricept® Oral Tablets in Healthy Male Volunteers

NCT ID: NCT05525780

Last Updated: 2023-07-13

Basic Information

• Recruitment Status: COMPLETED
• Clinical Phase: PHASE1
• Total Enrollment: 48 participants
• Study Classification: INTERVENTIONAL
• Study Start Date: 2022-08-26
• Study Completion Date: 2023-06-02

Brief Summary

This study is to evaluate the safety and tolerability of single dose of GB-5001 (donepezil) IM depot in healthy male volunteers. And, it is to predict the multiple-dose pharmacokinetics based on the single-dose pharmacokinetics of GB-5001 IM depot and the oral Aricept® (donepezil hydrochloride) tablet by PK modeling.

Conditions

Alzheimer Disease

Study Design

• Allocation Method: RANDOMIZED
• Intervention Model: SEQUENTIAL
• Primary Study Purpose: TREATMENT
• Blinding Strategy: QUADRUPLE

Study Groups

GB-5001

GB-5001 Suspension for intramuscular (IM) injection at three doses

Group Type: EXPERIMENTAL

GB-5001

Intervention Type: DRUG

Depending on the cohort, volume will be varied to administer.

Placebo

Placebo Suspension for intramuscular (IM) injection, Volume to be matched with the active drug in the respective cohort

Group Type: PLACEBO_COMPARATOR

Placebo

Intervention Type: DRUG

A matched volume of placebo product will be administered to each subject in each cohort.

Oral cohort

Aricept® tablet

Group Type: ACTIVE_COMPARATOR

Oral cohort

Intervention Type: DRUG

Single dose of Aricept tablet

Interventions

GB-5001

Depending on the cohort, volume will be varied to administer.

Intervention Type: DRUG

Placebo

A matched volume of placebo product will be administered to each subject in each cohort.

Intervention Type: DRUG

Oral cohort

Single dose of Aricept tablet

Intervention Type: DRUG

Eligibility Criteria

Inclusion Criteria

• Healthy, non-smoking male volunteers, 18-55 years of age, inclusive at the time of informed consent.
• Body mass index (BMI) that is within 18.5 - 30.0 kg/m2, inclusive, and weight at least 55 kg and above.
• Healthy, according to the medical history, ECG, vital signs, laboratory results and physical examination as determined by the PI/Sub-Investigator.
• Systolic blood pressure between 95-140 mmHg, inclusive, and diastolic blood pressure between 55-90 mmHg, inclusive, and heart rate between 60-100 bpm, inclusive, unless deemed otherwise by the PI/Sub-Investigator.
• Clinical laboratory values within the clinical site's most recent acceptable laboratory test range, and/or values are deemed by the PI/Sub-Investigator as "Not Clinically Significant".

Exclusion Criteria

• Known history or presence of any clinically significant hepatic, renal/genitourinary, gastrointestinal, cardiovascular, cerebrovascular, pulmonary, endocrine, immunological, musculoskeletal, neurological, psychiatric, dermatological or hematological disease or condition unless determined as not clinically significant by the PI/Sub-Investigator.
• Known history or presence of seizure or convulsion, unless determined as not clinically significant by the PI/Sub-Investigator.
• Known history or presence of peptic ulcer or gastrointestinal bleeding within 3 months prior to study drug administration, unless determined as not clinically significant by the PI/Sub-Investigator.
• Known risk of developing ulcers (for example, if you are taking non-steroidal anti-inflammatory drugs [NSAIDS] or high doses of acetylsalicylic acid [ASA] [Aspirin®]), unless determined as not clinically significant by the PI/Sub-Investigator.
• Clinically significant history or presence of any clinically significant gastrointestinal pathology (e.g., chronic diarrhea, inflammatory bowel disease), unresolved gastrointestinal symptoms, or other conditions known to interfere with the absorption, distribution, metabolism, or excretion of the drug experienced within 7 days prior to study drug administration, as determined by the PI/Sub-Investigator.
• Presence of any clinically significant illness within 30 days prior to dosing, as determined by the PI/Sub-Investigator
• Presence of any clinically significant illness within 30 days prior to dosing, as determined by the PI/Sub-Investigator.

• Minimum Eligible Age: 18 Years
• Maximum Eligible Age: 55 Years
• Eligible Sex: MALE
• Accepts Healthy Volunteers: Yes

Sponsors

G2GBio, Inc.

INDUSTRY

Sponsor Role: lead

Responsible Party

Responsibility Role: SPONSOR

Locations

Syneos Health

Québec, , Canada

Countries

Canada

References

Khwarg J, Lee H, Yu KS, Seol E, Chung JY. Population Pharmacokinetic Modeling and Simulation for Dose Optimization of GB-5001, a Long-Acting Intramuscular Injection of Donepezil, in Healthy Participants. Neurol Ther. 2024 Oct;13(5):1453-1466. doi: 10.1007/s40120-024-00643-4. Epub 2024 Aug 10.

Reference Type: DERIVED

PMID: 39126603 (View on PubMed)

Other Identifiers

G2GBio

Identifier Type: -

Identifier Source: org_study_id