A Study to Compare the Pharmacokinetics of BR4002 and BR4002-1 in Healthy Volunteers

NCT ID: NCT04462029

Last Updated: 2020-10-28

Study Results

Results pending

The study team has not published outcome measurements, participant flow, or safety data for this trial yet. Check back later for updates.

Basic Information

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Recruitment Status

COMPLETED

Clinical Phase

EARLY_PHASE1

Total Enrollment

18 participants

Study Classification

INTERVENTIONAL

Study Start Date

2020-06-05

Study Completion Date

2020-10-07

Brief Summary

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This study is designed as a randomized, open-label, single-dose, 6x3 crossover study.

Detailed Description

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A total of 18 subjects will be randomized into 6 sequence groups. The investigational products will be administered according to the treatment groups (R, T1, and T2) assigned to each sequence group in Period 1, Period 2, and Period 3. In between each period, there will be a washout period (28 days) long enough for the administered IP to be metabolized and eliminated.

Conditions

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Dementia Alzheimers

Study Design

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Allocation Method

RANDOMIZED

Intervention Model

CROSSOVER

Primary Study Purpose

TREATMENT

Blinding Strategy

NONE

Study Groups

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sequence 1

A total of 18 subjects will be randomized into 6 sequence groups. The investigational products (IPs) will be administered according to the treatment groups (R, T1, and T2) assigned to each sequence group in Period 1, Period 2, and Period 3. In between each period, there will be a washout period (28 days) long enough for the administered IP to be metabolized and eliminated.

* R(Reference): BR4002-1 (oral intake) 5mg single-dose
* T1(Test1): BR4002 (patch) 5mg single-dose (using the applicator)
* T2(Test2): BR4002 (patch) 5mg single-dose (not using the applicator)

sequence 1: R - T1 - T2

Group Type OTHER

BR4002

Intervention Type DRUG

* Administration to the T1 group: 5 mg of BR4002 (patch) will be attached using an applicator for 24 hours
* Administration to the T2 group: 5 mg of BR4002 (patch) will be attached without using an applicator for 24 hours

BR4002-1

Intervention Type DRUG

Administration to the R group: 5 mg of BR4002-1 (oral formulation) will be administered with 150 mL of water

sequence 2

A total of 18 subjects will be randomized into 6 sequence groups. The investigational products (IPs) will be administered according to the treatment groups (R, T1, and T2) assigned to each sequence group in Period 1, Period 2, and Period 3. In between each period, there will be a washout period (28 days) long enough for the administered IP to be metabolized and eliminated.

* R(Reference): BR4002-1 (oral intake) 5mg single-dose
* T1(Test1): BR4002 (patch) 5mg single-dose (using the applicator)
* T2(Test2): BR4002 (patch) 5mg single-dose (not using the applicator)

sequence 2: R - T2 - T1

Group Type OTHER

BR4002

Intervention Type DRUG

* Administration to the T1 group: 5 mg of BR4002 (patch) will be attached using an applicator for 24 hours
* Administration to the T2 group: 5 mg of BR4002 (patch) will be attached without using an applicator for 24 hours

BR4002-1

Intervention Type DRUG

Administration to the R group: 5 mg of BR4002-1 (oral formulation) will be administered with 150 mL of water

sequence 3

A total of 18 subjects will be randomized into 6 sequence groups. The investigational products (IPs) will be administered according to the treatment groups (R, T1, and T2) assigned to each sequence group in Period 1, Period 2, and Period 3. In between each period, there will be a washout period (28 days) long enough for the administered IP to be metabolized and eliminated.

* R(Reference): BR4002-1 (oral intake) 5mg single-dose
* T1(Test1): BR4002 (patch) 5mg single-dose (using the applicator)
* T2(Test2): BR4002 (patch) 5mg single-dose (not using the applicator)

sequence 3: T1 - R - T2

Group Type OTHER

BR4002

Intervention Type DRUG

* Administration to the T1 group: 5 mg of BR4002 (patch) will be attached using an applicator for 24 hours
* Administration to the T2 group: 5 mg of BR4002 (patch) will be attached without using an applicator for 24 hours

BR4002-1

Intervention Type DRUG

Administration to the R group: 5 mg of BR4002-1 (oral formulation) will be administered with 150 mL of water

sequence 4

A total of 18 subjects will be randomized into 6 sequence groups. The investigational products (IPs) will be administered according to the treatment groups (R, T1, and T2) assigned to each sequence group in Period 1, Period 2, and Period 3. In between each period, there will be a washout period (28 days) long enough for the administered IP to be metabolized and eliminated.

* R(Reference): BR4002-1 (oral intake) 5mg single-dose
* T1(Test1): BR4002 (patch) 5mg single-dose (using the applicator)
* T2(Test2): BR4002 (patch) 5mg single-dose (not using the applicator)

sequence 4: T1 - T2 - R

Group Type OTHER

BR4002

Intervention Type DRUG

* Administration to the T1 group: 5 mg of BR4002 (patch) will be attached using an applicator for 24 hours
* Administration to the T2 group: 5 mg of BR4002 (patch) will be attached without using an applicator for 24 hours

BR4002-1

Intervention Type DRUG

Administration to the R group: 5 mg of BR4002-1 (oral formulation) will be administered with 150 mL of water

sequence 5

A total of 18 subjects will be randomized into 6 sequence groups. The investigational products (IPs) will be administered according to the treatment groups (R, T1, and T2) assigned to each sequence group in Period 1, Period 2, and Period 3. In between each period, there will be a washout period (28 days) long enough for the administered IP to be metabolized and eliminated.

* R(Reference): BR4002-1 (oral intake) 5mg single-dose
* T1(Test1): BR4002 (patch) 5mg single-dose (using the applicator)
* T2(Test2): BR4002 (patch) 5mg single-dose (not using the applicator)

sequence 5: T2 - R - T1

Group Type OTHER

BR4002

Intervention Type DRUG

* Administration to the T1 group: 5 mg of BR4002 (patch) will be attached using an applicator for 24 hours
* Administration to the T2 group: 5 mg of BR4002 (patch) will be attached without using an applicator for 24 hours

BR4002-1

Intervention Type DRUG

Administration to the R group: 5 mg of BR4002-1 (oral formulation) will be administered with 150 mL of water

sequence 6

A total of 18 subjects will be randomized into 6 sequence groups. The investigational products (IPs) will be administered according to the treatment groups (R, T1, and T2) assigned to each sequence group in Period 1, Period 2, and Period 3. In between each period, there will be a washout period (28 days) long enough for the administered IP to be metabolized and eliminated.

* R(Reference): BR4002-1 (oral intake) 5mg single-dose
* T1(Test1): BR4002 (patch) 5mg single-dose (using the applicator)
* T2(Test2): BR4002 (patch) 5mg single-dose (not using the applicator)

sequence 6: T2 - T1 - R

Group Type OTHER

BR4002

Intervention Type DRUG

* Administration to the T1 group: 5 mg of BR4002 (patch) will be attached using an applicator for 24 hours
* Administration to the T2 group: 5 mg of BR4002 (patch) will be attached without using an applicator for 24 hours

BR4002-1

Intervention Type DRUG

Administration to the R group: 5 mg of BR4002-1 (oral formulation) will be administered with 150 mL of water

Interventions

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BR4002

* Administration to the T1 group: 5 mg of BR4002 (patch) will be attached using an applicator for 24 hours
* Administration to the T2 group: 5 mg of BR4002 (patch) will be attached without using an applicator for 24 hours

Intervention Type DRUG

BR4002-1

Administration to the R group: 5 mg of BR4002-1 (oral formulation) will be administered with 150 mL of water

Intervention Type DRUG

Eligibility Criteria

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Inclusion Criteria

1. Healthy adults aged ≥ 19 and ≤ 55 years at screening
2. Body weight of ≥ 50 kg with calculated body mass index (BMI) of ≥ 18.0 to ≤ 29.0 kg/m2
3. Determined eligible based on the results of physical examination and investigator questioning conducted according to this protocol. That is, absence of congenital or chronic disease, and absence of pathological symptoms or findings based on medical examination in the last 3 years.
4. Determined eligible based on the results of the laboratory tests and electrocardiogram (ECG) conducted according to this protocol
5. Voluntarily decided to participate in the study and provided written consent to follow precautions after receiving a detailed explanation on this study and fully understanding the information

Exclusion Criteria

1. Hypersensitivity to, or history of clinically significant hypersensitivity to donepezil hydrochloride, piperidine derivatives or any ingredients of piperidine derivatives, or other drugs (aspirin, antibiotics, etc.)
2. Hereditary disorders including galactose intolerance, Lapp lactase deficiency, and glucose-galactose malabsorption
3. History of heart disease such as sinus node syndrome, intra-atrial conduction disturbance or atrioventricular junctional conduction disturbance
4. Ongoing administration of non-steroidal anti-inflammatory drugs or history of peptic ulcer
5. History of asthma or obstructive pulmonary disease
6. Extrapyramidal disorder
7. Psychotic disorders or drug addiction
8. Presence or prior history of a gastrointestinal disorder or prior history of gastrointestinal surgery or skin graft that may affect the absorption of the IP
9. Presence or prior history of clinically significant cardiovascular, respiratory, hepatic, renal, neurological, endocrine, hematological and oncological, psychotic, or urinary disease
10. Clinically significant hypotension (systolic blood pressure \< 90 mmHg) or hypertension (systolic blood pressure ≥ 150 mmHg or diastolic blood pressure ≥ 95 mmHg) at screening
11. Any of the following results from screening tests:

* AST or ALT \> 2 times the upper limit of normal
* Total bilirubin \> 2.0 mg/dL
* Estimated glomerular filtration rate (eGFR) \< 60 mL/min/1.73m2
12. QTc \> 450 ms or any clinically significant abnormal finding from an ECG result at screening
13. Continuous alcohol intake or inability to stop drinking during the study period
14. Continuous smoking or inability to stop smoking throughout the hospitalization during the study period
15. Participated in another clinical study or bioequivalence study within 6 months prior to the first administration of the IP
16. Donated whole blood within 60 days or blood components within 30 days, or received blood transfusion within 30 days prior to the first administration of the IP
17. Used any prescription drugs or herbal medicines within 14 days, or any over-the-counter (OTC) drugs within 7 days prior to the first administration of the IP
18. Used drugs inducing and inhibiting drug-metabolizing enzymes, such as barbitals, within 1 month prior to initiation of the study
19. Have been on a diet (especially grapefruit juice or its product) which may affect absorption, distribution, metabolism, and excretion of the drug within 7 days prior to the first administration of the IP
20. Do not agree to exclude the possibility of pregnancy by using medically acceptable methods of contraception from the first day of administration of the IP up to 7 days after the last day of administration of the IP
21. Unwillingness or inability to comply with the diet and lifestyle guidelines required for the study
22. Clinically significant abnormal laboratory results or considered ineligible for study participation by the investigator for any other reason
23. Women who are pregnant, have a positive serum/urine hCG test, or are breastfeeding
Minimum Eligible Age

19 Years

Maximum Eligible Age

55 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

Yes

Sponsors

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Boryung Pharmaceutical Co., Ltd

INDUSTRY

Sponsor Role lead

Responsible Party

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Responsibility Role SPONSOR

Principal Investigators

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Sang-Heon Cho

Role: PRINCIPAL_INVESTIGATOR

Inha University Hospital

Locations

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Inha University Hospital

Incheon, , South Korea

Site Status

Countries

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South Korea

Other Identifiers

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BR-DPZ-CT-102

Identifier Type: -

Identifier Source: org_study_id