Pharmacokinetic Study of Levocetirizine Oral Solution

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details. Identifier: NCT01622283
Recruitment Status : Completed
First Posted : June 19, 2012
Last Update Posted : June 12, 2017
Information provided by (Responsible Party):

Brief Summary:

This study will be a single center, open-label, randomized, single dose, in the fasted condition and 2-way crossover study to evaluate the pharmacokinetics, the safety and tolerability of levocetirizine oral solution 5 mg and cetirizine dry syrup 10 mg in Japanese healthy male subjects.

Approximately 20 subjects will receive both treatments of levocetirizine oral solution 5 mg and cetirizine dry syrup 10 mg in the design. Serial pharmacokinetic samples will be collected and safety assessments will be performed following each dose.

The primary objective of the study is to demonstrate the bioequivalence of levocetirizine in plasma, when given as levocetirizine oral solution 5 mg relative to cetirizine DS 10 mg in Japanese healthy male subjects.

Condition or disease Intervention/treatment Phase
Rhinitis, Allergic, Perennial and Seasonal Drug: Levocetirizine Drug: Cetirizine Phase 1

Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 20 participants
Allocation: Randomized
Intervention Model: Crossover Assignment
Masking: None (Open Label)
Primary Purpose: Other
Official Title: Pharmacokinetic Study of Levocetirizine Oral Solution-An Open-label, Randomized, Cross-over Study to Evaluate the Pharmacokinetics, the Safety and Tolerability of Levocetirizine Oral Solution (5 mg) and Cetirizine Dry Syrup (10 mg), Following a Single Dose in Japanese Healthy Male Subjects-
Actual Study Start Date : May 2, 2012
Actual Primary Completion Date : June 10, 2012
Actual Study Completion Date : June 10, 2012

Arm Intervention/treatment
Experimental: Levocetirizine oral solution 5 mg
Levocetirizine oral solution 5 mg
Drug: Levocetirizine
Active Comparator: Cetirizine dry syrup 10 mg
Cetirizine dry syrup 10 mg
Drug: Cetirizine

Primary Outcome Measures :
  1. AUC(0-48) of levocetirizine [ Time Frame: pre, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48h post dose ]
    AUC(0-48): Area under plasma concentration time curve from pre-dose to 48h.

  2. Cmax of levocetirizine [ Time Frame: pre, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48h post dose ]
    Cmax: Maximum observed concentration.

Secondary Outcome Measures :
  1. Adverse events [ Time Frame: up to 48h post dose ]
    Number of participants with adverse events as a measure of safety and tolerability.

  2. Safety and tolerability [ Time Frame: up to 48h post dose ]
    Safety and tolerability of levocetirizine and cetirizine in terms of clinical laboratory tests, vital sign, body weight and ECG.

  3. Vital sign [ Time Frame: up to 48h post dose ]
    Systolic and diastolic blood pressure, body temperature and pulse rate.

  4. Body weight [ Time Frame: up to 48h post dose ]
  5. ECG [ Time Frame: up to 48h post dose ]
    Heart rate, PR, QRS, QT, and QTc intervals.

  6. Laboratory tests [ Time Frame: up to 48h post dose ]
    Clinical Chemistry (Total Protein, Albumin, Total and Direct Bilirubin, BUN, Creatinine, Uric Acid, TG, Total Cholesterol, LDL and HDL-cholesterol, AST, ALT, Alkaline Phosphatase, LDH, GGT, CPK, Amylase, Glucose(fasting), Sodium, Potassium, Chloride, Calcium, Phosphorus), Hematology (Platelet Count, RBC Count, WBC Count (absolute), Reticulocyte Count, Hemoglobin, Hematocrit, RBC Indices (MCV, MCH, MCHC) and Automated WBC Differential (Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils)) and Urinalysis (Specific Gravity, pH, Glucose, Protein, Blood, Ketones and Microscopic Examination)

  7. AUC(0-inf), MRT, tmax, and t1/2 of levocetirizine [ Time Frame: pre, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48h post dose ]
    AUC(0-inf): Area under the concentration-time curve from time pre-dose extrapolated to infinite time, MRT: Mean residence time, tmax: Time of occurrence of Cmax, and t1/2: Terminal phase half-life.

Information from the National Library of Medicine

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Ages Eligible for Study:   20 Years to 55 Years   (Adult)
Sexes Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes

Inclusion Criteria:

  • Healthy as determined by a responsible and experienced physician, based on a medical evaluation including medical history, physical examination, laboratory tests and cardiac monitoring. A subject with a clinical abnormality or laboratory parameters outside the reference range for the population being studied may be included only if the Investigator and the GSK Medical Monitor agree that the finding is unlikely to introduce additional risk factors and will not interfere with the study procedures.
  • Japanese male between 20 and 55 years of age inclusive, at the time of signing the informed consent.
  • Non-smoker or ex-smoker having ceased smoking for at least 6 months.
  • Body weight => 50 kg and BMI within the range 18.5 - 25.0 kg/m2 at screening.
  • A signed and dated written informed consent is obtained from the subject.
  • Able to complete all study procedures and planned treatment periods.
  • ALT, alkaline phosphatase and bilirubin =< 1.5xULN (isolated bilirubin > 1.5xULN is acceptable if bilirubin is fractionated and direct bilirubin < 35%).
  • Single QTcB < 450 msec at screening.

Exclusion Criteria:

  • The subject is positive for syphilis, Hepatitis B surface antigen, Hepatitis C antibody, HIV1/2 antibody, or HTLV-1 antibody at screening.
  • Current or chronic history of liver disease, or known hepatic or biliary abnormalities (with the exception of Gilbert's syndrome or asymptomatic gallstones).
  • The subject has a history of allergic rhinitis.
  • 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.
  • The subject has a history or current conditions of drug abuse or alcoholism.
  • A positive pre-study drug screen.
  • History of regular alcohol consumption within 6 months of the study defined as an average weekly intake of >14 drinks. One drink is equivalent to 12 g of alcohol: 12 ounces (350 mL) of beer, 5 ounces (150 mL) of wine or 1.5 ounces (45 mL) of 80 proof distilled spirits.
  • The subject has participated in a clinical trial and has received an investigational product or a non-investigational drug within 4 months prior to the first dosing day in the current study.
  • Exposure to more than four new chemical entities within 12 months prior to the first dosing day.
  • Unable to refrain from the use of prescription or non-prescription drugs, including vitamins, herbal and dietary supplements (including St John's Wort) within 14 days or 5 half-lives (whichever is longer) prior to the first dose of study medication, unless in the opinion of the Investigator and GSK Medical Monitor the medication will not interfere with the study procedures or compromise subject safety.
  • History of sensitivity to any of the study medications, or components thereof or a history of drug or other allergy.
  • Where participation in the study would result in donation of blood or blood products => 400 mL within 3 months or => 200 mL within 1 month.
  • Unwillingness or inability to follow the procedures outlined in the protocol.
  • Subject is mentally or legally incapacitated.

Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its identifier (NCT number): NCT01622283

GSK Investigational Site
Kagoshima, Japan, 890-0081
Sponsors and Collaborators
Study Director: GSK Clinical Trials GlaxoSmithKline

Additional Information:
Publications automatically indexed to this study by Identifier (NCT Number):
Responsible Party: GlaxoSmithKline Identifier: NCT01622283     History of Changes
Other Study ID Numbers: 116459
First Posted: June 19, 2012    Key Record Dates
Last Update Posted: June 12, 2017
Last Verified: June 2017

Additional relevant MeSH terms:
Rhinitis, Allergic
Rhinitis, Allergic, Perennial
Nose Diseases
Respiratory Tract Diseases
Respiratory Tract Infections
Otorhinolaryngologic Diseases
Respiratory Hypersensitivity
Hypersensitivity, Immediate
Immune System Diseases
Pharmaceutical Solutions
Anti-Allergic Agents
Histamine H1 Antagonists, Non-Sedating
Histamine H1 Antagonists
Histamine Antagonists
Histamine Agents
Neurotransmitter Agents
Molecular Mechanisms of Pharmacological Action
Physiological Effects of Drugs