Pharmacokinetic Study of Levocetirizine Oral Solution

This study has been completed.
Sponsor:
Information provided by (Responsible Party):
GlaxoSmithKline
ClinicalTrials.gov Identifier:
NCT01622283
First received: April 19, 2012
Last updated: July 19, 2012
Last verified: June 2012
  Purpose

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 Intervention Phase
Rhinitis, Allergic, Perennial and Seasonal
Drug: Levocetirizine
Drug: Cetirizine
Phase 1

Study Type: Interventional
Study Design: Allocation: Randomized
Endpoint Classification: Bio-equivalence Study
Intervention Model: Crossover Assignment
Masking: Open Label
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-

Resource links provided by NLM:


Further study details as provided by GlaxoSmithKline:

Primary Outcome Measures:
  • 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 ] [ Designated as safety issue: No ]
    AUC(0-48): Area under plasma concentration time curve from pre-dose to 48h.

  • 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 ] [ Designated as safety issue: No ]
    Cmax: Maximum observed concentration.


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

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

  • Vital sign [ Time Frame: up to 48h post dose ] [ Designated as safety issue: Yes ]
    Systolic and diastolic blood pressure, body temperature and pulse rate.

  • Body weight [ Time Frame: up to 48h post dose ] [ Designated as safety issue: Yes ]
  • ECG [ Time Frame: up to 48h post dose ] [ Designated as safety issue: Yes ]
    Heart rate, PR, QRS, QT, and QTc intervals.

  • Laboratory tests [ Time Frame: up to 48h post dose ] [ Designated as safety issue: Yes ]
    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)

  • 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 ] [ Designated as safety issue: No ]
    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.


Enrollment: 20
Study Start Date: May 2012
Study Completion Date: June 2012
Primary Completion Date: June 2012 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: Levocetirizine oral solution 5 mg
Levocetirizine oral solution 5 mg
Drug: Levocetirizine
Levocetirizine
Active Comparator: Cetirizine dry syrup 10 mg
Cetirizine dry syrup 10 mg
Drug: Cetirizine
Cetirizine

  Eligibility

Ages Eligible for Study:   20 Years to 55 Years
Genders Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes
Criteria

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.
  Contacts and Locations
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the Contacts provided below. For general information, see Learn About Clinical Studies.

Please refer to this study by its ClinicalTrials.gov identifier: NCT01622283

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

No publications provided

Responsible Party: GlaxoSmithKline
ClinicalTrials.gov Identifier: NCT01622283     History of Changes
Other Study ID Numbers: 116459
Study First Received: April 19, 2012
Last Updated: July 19, 2012
Health Authority: Japan: Ministry of Health, Labor and Welfare

Additional relevant MeSH terms:
Rhinitis
Rhinitis, Allergic, Perennial
Nose Diseases
Respiratory Tract Diseases
Respiratory Tract Infections
Otorhinolaryngologic Diseases
Respiratory Hypersensitivity
Hypersensitivity, Immediate
Hypersensitivity
Immune System Diseases
Pharmaceutical Solutions
Cetirizine
Levocetirizine
Therapeutic Uses
Pharmacologic Actions
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

ClinicalTrials.gov processed this record on September 14, 2014