Human Mass Balance Study With Bilastine

Primary Endpoints are: Whole blood and plasma concentrations of total radioactivity and parent drug. Urine and faecal recovery of total radioactivity. Characterisation and identification of metabolites in plasma, urine and faeces.

Inclusion criteria

• No clinically important abnormal physical findings.
• No clinically significant abnormalities in the results of laboratory evaluation.
• Normal ECG.
• Normal supine blood pressure and heart rate.
• Body weight between 50 and 100 kg and body mass index between 18 and 30 kg/m2.
• Able to communicate well with the investigator and to comply with the requirements of the entire study.
• Provision of written informed consent to participate.
• Subjects must agree to use an adequate method of contraception during the study and for 12 weeks after dosing.
• Subjects must have a negative urine screen for drugs of abuse.
• Subjects must have a regular bowel habit.

Exclusion criteria

• Administration of any IMP within 12 weeks before entry to the study.
• Use of any prescribed medication or St John's Wort within 14 days or OTC medication within 5 days of dosing.
• Existence of any surgical or medical condition which, in the judgement of the investigator, might interfere with the absorption, distribution, metabolism or excretion of the IMP.
• History of any drug or alcohol abuse in the past 2 years, or alcohol consumption greater than 21 units per week.
• Presence or history of allergy requiring treatment.
• Hayfever is allowed unless it is active or has required treatment within the previous 2 months.
• Donation or loss of greater than 400 mL of blood within 12 weeks before entry to the study.
• Serious adverse reaction or serious hypersensitivity to any drug.
• Presence of hepatitis B surface antigen (HBsAg), hepatitis C antibody (HCV Ab) or HIV 1 or HIV 2 antibodies at screening.
• Administration of radiolabelled substances or exposure to significant radiation (eg serial x-ray or CT scans, barium meal etc) within the past 12 months.
• Any ECG abnormality at screening (including QTc intervals of >430 ms).
• Past medical history of clinically significant ECG abnormalities, or a family history of a prolonged QT interval syndrome.
• Abnormal diet or substantial changes in eating habits within 30 days prior to study initiation.
• Treatment with any known enzyme altering agents (barbiturates, phenothiazines, cimetidine, etc.) within 2 months prior to or during the study.