Different Level of Single-dose and Multiple-dose Bilastine PK Study in Chinese Population

A Different Level of Single-dose and Multiple-dose Study to Evaluate the Pharmacokinetics of Bilastine in a Chinese Population

This is a single-dose and multiple-dose, open-label, single-centre pharmacokinetic (PK) study which will be conducted in Phase I Clinical Trial Centre, Chinese University of Hong Kong, to evaluate pharmacokinetics (PK) of different levels of single-dose and multiple-dose of bilastine in healthy Chinese subjects.

Study Overview

• Status: Unknown
• Conditions: Pharmacokinetics
• Intervention / Treatment: Drug: Bilastine 40mg single dose; Drug: Bilastine 20mg single-dose followed by multiple-dose

Detailed Description

This is a single-dose and multiple-dose, open-label, single-centre pharmacokinetic (PK) study, to evaluate pharmacokinetics (PK) of different levels of single-dose and multiple-dose of bilastine in healthy Chinese subjects. Total 24 subjects will be enrolled into the study and divided into 2 cohorts, 12 subjects in each cohort.

Single-dose only cohort treatment duration is 1 day and receive a single dose of 40 mg of bilastine then collect PK blood sample. Single-dose followed by multiple-dose cohort treatment duration of this cohort is 9 days. Subjects will receive a single dose of bilastine 20 mg on the morning of Day 1; and six doses of bilastine 20 mg in the morning from Day 4 to Day 9 and collect PK blood samples. The primary objective of the study is to determine the PK properties of orally administered bilastine in healthy Chinese population. The secondary objective of the study is to evaluate the safety and tolerability of bilastine administered as a single and multiple doses in healthy Chinese subjects.

• Study Type: Interventional
• Enrollment (Anticipated): 24
• Phase: Phase 1

Contacts and Locations

• Study Contact: Name: Maria Carolina De Quiroz, MD; Phone Number: +65 6494 7226; Email: carolina.dequiroz@menariniapac.com

Study Locations

• China
  • Hong Kong
    • Hong Kong, Hong Kong, China, 999077
      • Recruiting
      • Phase I Clinical Trial Centre, Chinese University of Hong Kong
      • Contact: Andrea Luk, Professor

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 45 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

1. Ethnic Chinese males and females between 18 and 45 years of age (inclusive).
2. Having voluntarily given their informed consent to participate in the study after receiving information about the design, aims and potential risks that could result from the study and being informed that they could refuse to take part in or withdraw from the study at any time.
3. Body mass of no less than 50 kg. Body mass index: 19 to 24 kg/m2 (inclusive).
4. No clinically significant abnormal findings from the physical examination, vital signs check, electrocardiogram (ECG), medical history, or clinical laboratory results during screening and pre-dosing of Day 1.
5. A negative screen for HIV and hepatitis B.
6. A negative urine or breathalyzer screen for alcohol and negative urine screen for drugs of abuse.
7. Are non-tobacco / nicotine users (within 3 months prior to screening visit).
8. A negative serum pregnancy test for female subjects.

9. Subjects who are willing to comply with the contraception restrictions for this study:

   1. True abstinence.
   2. Barrier methods with spermicidal use. The use of barrier contraceptives should always be supplemented with the use of a spermicide, where available.
   3. Intrauterine devices: intrauterine device with the use of condom or spermicide.
   4. Sterilization of male subjects (with the appropriate post-vasectomy documentation of the absence of sperm in the ejaculate).

Exclusion Criteria:

1. History of clinically significant gastrointestinal, renal, hepatic, neurologic, haematological, endocrine, oncologic, pulmonary, immunologic, psychiatric, or cardiovascular disease or any other condition which, in the opinion of the Investigator, jeopardises the safety of the subject or will impact the validity of the study results.
2. History of allergic or adverse response to antihistamine drugs.
3. Participated in a clinical trial within 90 days prior to screening.
4. Donated blood within 90 days prior to screening.
5. Donated plasma within 90 days prior to screening.
6. Abnormal diet or substantial changes in eating habits within 30 days prior to screening.
7. Used any prescription medication within 14 days prior to or during screening, especially any known P-glycoprotein transporter inhibitors agents (ketoconazole, erythromycin, ciclosporin, digoxin, etc.).
8. Used any prescription or any over-the-counter medication, herbal or traditional Chinese medication within 7 days prior to or during screening.
9. Intake of grapefruit or any other citrus fruit, fruit juice or cranberries within 72 hours prior to study drug administration.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Non-Randomized
• Interventional Model: Sequential Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Bilastine 40mg single dose; 12 eligible subjects will be allocated to this arm and receive a single dose of 40 mg of bilastine	Drug: Bilastine 40mg single dose; Single-dose only cohort treatment duration is 1 day. After the screening period, eligible subjects will be allocated to receive a single dose of 40 mg of bilastine
Experimental: Bilastine 20mg multiple dose; 12 eligible subjects will be allocated to this arm and receive a single dose of bilastine 20 mg on Day 1 and six doses of bilastine 20 mg from Day 4 to Day 9	Drug: Bilastine 20mg single-dose followed by multiple-dose; Single-dose followed by multiple-dose cohort treatment duration of this cohort is 9 days. Subjects will receive a single dose of bilastine 20 mg on the morning of Day 1; and six doses of bilastine 20 mg in the morning from Day 4 to Day 9.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Pharmacokinetic (Cmax)	observed maximum plasma concentration	day1, day4 to day9
Pharmacokinetic (tmax)	time to reach Cmax	day1, day4 to day9
Pharmacokinetic (λz)	terminal rate constant	day1, day4 to day9
Pharmacokinetic (t½)	terminal half-life	day1, day4 to day9
Pharmacokinetic [AUC(0-24)]	area under the plasma concentration-time curve from zero to 24 hours after study drug administration	day1
Pharmacokinetic [AUC(0-last)]	from time zero to the time of last quantifiable concentration	day1
Pharmacokinetic [AUC(0-inf)]	from time zero extrapolated to infinity	day1
Pharmacokinetic (CL/F)	apparent systemic clearance following oral dosing	day1, day4 to day9
Pharmacokinetic (Vz/F)	apparent volume of distribution during terminal phase following oral dosing	day1, day4 to day9
Pharmacokinetic [AUC(0-inf)/D]	dose-normalized AUC(0-inf)	day1
Pharmacokinetic (Cmax/D)	dose-normalized Cmax	day1
Pharmacokinetic (Cavg)	average concentration over the study drug interval	day4 to day9
Pharmacokinetic [AUC(0-tau)]	area under the plasma concentration-time curve during the dosing interval following multiple dosing	day4 to day9
Pharmacokinetic (FI)	fluctuation index	day4 to day9
Pharmacokinetic (LI)	linearity index	day4 to day9
Pharmacokinetic [RAUC(0-tau)]	accumulation ratio for AUC(0-tau)	day4 to day9
Pharmacokinetic (RCmax)	accumulation for Cmax	day4 to day9

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Adverse events	Safety will be evaluated with summary of Adverse Events	day1 to day16

Collaborators and Investigators

• Sponsor: A.Menarini Asia-Pacific Holdings Pte Ltd
• Investigators: Principal Investigator: Andrea Luk, Professor, Phase I Clinical Trial Centre, Chinese University of Hong Kong

Study record dates

Study Major Dates

• Study Start (Actual): August 28, 2018
• Primary Completion (Anticipated): April 30, 2019
• Study Completion (Anticipated): July 31, 2019

Study Registration Dates

• First Submitted: August 3, 2018
• First Submitted That Met QC Criteria: August 14, 2018
• First Posted (Actual): August 16, 2018

Study Record Updates

• Last Update Posted (Actual): January 10, 2019
• Last Update Submitted That Met QC Criteria: January 8, 2019
• Last Verified: August 1, 2018

More Information

Terms related to this study

• Other Study ID Numbers: INCN/12/Bil-PK/004

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No