Bioavailability of 5 mg of Levamlodipine Maleate Tablets Versus 10 mg of Amlodipine Besylate Tablet in Healthy Subjects

NCT03657550 | Completed Phase 1 FDA Drug

• 1 other identifier: LAM-US-101
• Study Type: interventional
• Target: 36
• Locations: 1 country
• Sites: 1

Brief Summary

This study are (1) to assess the relative bioavailability (BA) of a single oral dose of either 5 mg of Levamlodipine Maleate Tablets from CSPC or 10 mg of Amlodipine Besylate Tablet (NORVASC®) from Pfizer Inc. under fasting condition in male and female healthy subjects; and (2) to evaluate food effect on the PK profile of Levamlodipine Maleate Tablets from CSPC.

Conditions

Hypertension

Outcome Measures

Primary Outcomes (1)

• The plasma concentration of study drugs

  Plasma concentration of study drugs will be measured at all the time points.

  6 weeks

Study Arms (2)

Test Drug - Reference Product - Test Drug (Food Effect)

OTHER

In Part 1, this group of subjects were treated with a single dose of 5 mg levamlodipine maleate tablets (Test Product), then crossed over to receive a single dose of 10 mg Amlodipine Besylate Tablet NORVASC® (Reference Product) under fasted conditions. After a wash-out period for 14-days, all subjects were rolled over to Part 2 where they received a single dose of 5 mg levamlodipine maleate tablets under a high-fat/high-calorie meal to assess food effect.

Drug: Levamlodipine, Amlodipine; Drug: Amlodipine, Levamlodipine

Reference Product - Test Drug - Test Drug (Food Effect)

OTHER

In Part 1, this group of subjects were treated with a single dose of 10 mg Amlodipine Besylate Tablet NORVASC® (Reference Product), and then crossed over to receive a single dose of 5 mg levamlodipine maleate tablets (Test Product) under fasted conditions. After a wash-out period for 14-days, all subjects were rolled over to Part 2 where they received a single dose of 5 mg levamlodipine maleate tablets under a high-fat/high-calorie meal to assess food effect.

Drug: Levamlodipine, Amlodipine; Drug: Amlodipine, Levamlodipine

Interventions

Levamlodipine, Amlodipine DRUG

In Part 1, this group of subjects were treated with a single dose of 5 mg levamlodipine maleate tablets (Test Product), then crossed over to receive a single dose of 10 mg Amlodipine Besylate Tablet NORVASC® (Reference Product) under fasted conditions. After a wash-out period for 14-days, all subjects were rolled over to Part 2 where they received a single dose of 5 mg levamlodipine maleate tablets under a high-fat/high-calorie meal to assess food effect.

Also known as: Xuanning®, NORVASC®

Reference Product - Test Drug - Test Drug (Food Effect); Test Drug - Reference Product - Test Drug (Food Effect)

Amlodipine, Levamlodipine DRUG

In Part 1, this group of subjects were treated with a single dose of 10 mg Amlodipine Besylate Tablet NORVASC® (Reference Product), and then crossed over to receive a single dose of 5 mg levamlodipine maleate tablets (Test Product) under fasted conditions. After a wash-out period for 14-days, all subjects were rolled over to Part 2 where they received a single dose of 5 mg levamlodipine maleate tablets under a high-fat/high-calorie meal to assess food effect.

Also known as: NORVASC®, Xuanning®

Reference Product - Test Drug - Test Drug (Food Effect); Test Drug - Reference Product - Test Drug (Food Effect)

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Women of childbearing potential (WOCBP) must have a negative pregnancy test at Screening and be practicing a medically acceptable method of contraception with an annual failure rate of less than 1% during the study and 60 days after discontinuation of study treatment.
• Considered healthy by the Principal Investigator, based on a detailed medical history, full physical examination, clinical laboratory tests, 12-lead ECG and vital signs;
• Nonsmoker, defined as not having smoked or used any form of tobacco in more than 6 months before screening;
• Body mass index (BMI) of 19 to 30 kg/m2 inclusive and body weight not less than 50 kg;

You may not qualify if:

• Clinically significant history of gastrointestinal, cardiovascular, musculoskeletal, endocrine, hematologic, psychiatric, renal, hepatic, bronchopulmonary, neurologic, immunologic, lipid metabolism disorders, or drug hypersensitivity;
• Mean systolic blood pressure of three measurements \>140 mmHg, or a mean diastolic blood pressure of three measurements \>90 mmHg at screening.
• Known or suspected malignancy;
• Positive blood screen for human immunodeficiency virus (HIV), or hepatitis B surface antigen (HBsAg), or hepatitis C virus (HCV);
• A history of seizure. However, a history of febrile seizure is allowed;
• Positive pregnancy test result, or plan to become pregnant if female;
• A hospital admission or major surgery within 30 days prior to screening;
• Participation in any other investigational drug trial within 30 days prior to screening;
• DSM-V substance use disorder within 6 months prior to screening;
• A positive result for alcohol or drugs of abuse at screening or admission;
• Tobacco use within 6 months prior to screening;
• An unwillingness or inability to comply with food and beverage restrictions during study participation;
• Donation or blood collection of more than 1 unit (approximate 450 mL) of blood (or blood products) or acute loss of blood during the 90 days prior to screening;
• Use of prescription or over-the-counter (OTC) medications, and herbal medicines (including St John's Wort, herbal teas, garlic extracts) within 14 days prior to dosing;
• A history of suicide attempt in the past 12 months and/or seen by the investigator as having a significant history of risk of suicide or homicide;

Sponsors & Collaborators

• Conjupro Biotherapeutics, Inc.: lead
• CSPC Ouyi Pharmaceutical Co., Ltd.: collaborator

Study Sites (1)

Collaborative Neuroscience Network, LLC

Long Beach, California, 90806, United States

Location

MeSH Terms

Conditions

Hypertension

Interventions

levamlodipine; Amlodipine

Condition Hierarchy (Ancestors)

Vascular Diseases; Cardiovascular Diseases

Intervention Hierarchy (Ancestors)

Dihydropyridines; Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

Study Officials

• Study Officials

  Conjupro Biotherapeutics, Inc.

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: This study consists of 2 parts. Part 1 will be a randomized, open-label, single-dose, two-way crossover study to assess the relative BA of levamlodipine maleate tablets from CSPC versus Amlodipine Besylate Tablet NORVASC® from Pfizer Inc. after a single oral administration under fasted conditions in male and female healthy subjects. Part 2 will be a single-arm, open-label, single-dose phase to assess food effect on the PK profile of levamlodipine maleate tablets from CSPC. Subjects who have completed Part 1 will be rolled over to Part 2 after a wash-out period for at least 14-days since the last dosing. Subjects will receive a single oral administration of study drug under a high-fat / high-calorie meal that should derive approximately 150, 250 and 500-600 calories from protein, carbohydrate and fat, respectively.

Study Record Dates

• First Submitted: June 21, 2018
• First Posted: September 5, 2018
• Study Start: May 31, 2018
• Primary Completion: September 6, 2018
• Study Completion: September 6, 2018
• Last Updated: September 16, 2021

Record last verified: 2018-09

Locations

US (1)