Phase 1 Study of Levocetirizine

A Single Blind, Randomized, Single Oral Dose Study to Compare the Oral Disposition of Levocetirizine When Given Alone (5mg) or as the Racemate (Cetirizine 10mg), and to Investigate the Safety and Tolerability and the Pharmacokinetics of Levocetirizine and Cetirizine, Following a Single Dose in Healthy Japanese Male Subjects

This is a single center, single blind, single dose, randomized, partial cross-over study to confirm bioequivalence between levocetirizine and cetirizine.

Study Overview

• Status: Completed
• Conditions: Dermatitis
• Intervention / Treatment: Drug: placebo; Drug: levocetirizine; Drug: cetirizine

• Study Type: Interventional
• Enrollment (Actual): 20
• Phase: Phase 1

Contacts and Locations

Study Locations

• Japan
  • Kagoshima, Japan, 890-0081
    • GSK Investigational Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 20 years to 64 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

1. Japanese healthy male subjects aged between 20 and 64 years of age inclusive. Healthy subjects are defined as individuals who are free from clinically significant illness or disease as determined by their medical history, physical examination, laboratory studies, and other tests.
2. Body weight ≥ 50 kg and BMI within the range 18.50-25.00 kg/m2 inclusive.
3. Non-smokers (at least 6 months).

4. Clinical laboratory tests data obtained at screening meet the following:

   AST(GOT), ALT(GPT), total-bilirubin, BUN, creatinine, uric acid,: below the upper normal range

5. Normal 12-lead EGC finding at screening; QTc interval <450msec
6. Capable of giving written informed consent, which includes compliance with the requirements and restrictions listed in the consent form.

Exclusion Criteria:

1. The subject has any clinically relevant abnormality on medical examination, vital sign, clinical laboratory test or medical history at screening in the medical opinion of the investigator or the subject has a medical history that is not considered as eligible for inclusion in this study by the investigator.
2. The subject has an allergy for any drug or idiosyncrasy.
3. The subject has a history of allergic rhinitis.
4. The subject has a history or presence of clinically significant gastrointestinal, hepatic or renal disease or other condition known to interfere with absorption, distribution, metabolism or elimination of drugs.
5. The subject is currently participating in another clinical study or post-marketing study in which the subject is or will be exposed to an investigational or a non-investigational drug or device.
6. The subject has participated in a clinical study with an investigational or a non-investigational drug or device during the previous 4 months.
7. The subject has a history or current conditions of drug abuse or alcoholism.
8. History of regular alcohol consumption exceeding on average, 14 drinks/week (1 drink = 150mL of wine or 360mL of beer or 45mL of 80 proof distilled spirits).
9. The subject is positive for urine drug screening.
10. The subject is positive for syphilis, HBs antigen, HCV antibody, HIV antibody, HTLV-1 antibody.
11. The subject has donated a unit of blood ">400mL" within the previous 4 months or ">200mL" within the previous 1 month.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Prevention
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: Single

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Other: levocetirizine; Study Drug	Drug: levocetirizine; levocetirizine
Other: cetirizine; Study Drug	Drug: cetirizine; cetiridine
Other: placebo; Study Drug	Drug: placebo; placebo

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
AUC0-48 of levocetirizine	Area Under the time-concentlation curve	predose,0.25,0.5,1,1.5,2,3,4,6,9,12,16,24,36, 48 hours post-dose
Cmax of levocetirizine	maximum concentration	predose,0.25,0.5,1,1.5,2,3,4,6,9,12,16,24,36, 48 hours post-dose

Secondary Outcome Measures

Outcome Measure	Time Frame
Number of Adverse events	predose,1,24 48 hours post-dose
Changes in clinical laboratory tests	predose,24,48 hours post-dose
Changes in vital signs	predose,1,24,48 hours post-dose
Changes in 12-lead ECG.	predose,1,24,48 hours post-dose

Collaborators and Investigators

• Sponsor: GlaxoSmithKline

Publications and helpful links

General Publications

• Hiroko Ino, Shigeru Nohda, Shuji Miki, Kastutoshi Hara, Toshiyasu Hirama. Comparison of levocetirizine pharmacokinetics, following a single dose of levocetirizine alone or as cetirizine in Japanese healthy male volunteers . [Jpn J Clin Pharmacol Therapeut]. 2010;41(6):309.

Study record dates

Study Major Dates

• Study Start (Actual): March 18, 2008
• Primary Completion (Actual): April 30, 2008
• Study Completion (Actual): April 30, 2008

Study Registration Dates

• First Submitted: June 23, 2011
• First Submitted That Met QC Criteria: May 14, 2015
• First Posted (Estimate): May 18, 2015

Study Record Updates

• Last Update Posted (Actual): August 3, 2017
• Last Update Submitted That Met QC Criteria: August 1, 2017
• Last Verified: August 1, 2017

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Skin Diseases; Dermatitis; Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Anti-Allergic Agents; Histamine H1 Antagonists; Histamine Antagonists; Histamine Agents; Histamine H1 Antagonists, Non-Sedating; Cetirizine; Levocetirizine
• Other Study ID Numbers: 111580