Human Mass Balance Study With Bilastine

NCT ID: NCT00572611

Last Updated: 2012-09-26

Basic Information

• Recruitment Status: COMPLETED
• Clinical Phase: PHASE1
• Total Enrollment: 6 participants
• Study Classification: INTERVENTIONAL
• Study Start Date: 2007-11-30
• Study Completion Date: 2007-12-31

Brief Summary

The primary objective of the study is to define the absorption and excretion kinetics of bilastine in man following oral administration, and to investigate the nature of the metabolites present in plasma and excreta. The secondary objective of the study is to assess the safety and tolerability of bilastine

Detailed Description

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.

Conditions

Healthy

Keywords

Mass Balance; Metabolism; Absorption; Excretion; Pharmacokinetics

Study Design

• Allocation Method: NA
• Intervention Model: SINGLE_GROUP
• Primary Study Purpose: BASIC_SCIENCE
• Blinding Strategy: NONE

Study Groups

I

Single oral dose of 20 mg \[14C\]-bilastine

Group Type: EXPERIMENTAL

[14C]-bilastine

Intervention Type: DRUG

Single oral dose of 20 mg \[14C\]-bilastine. 1 capsule. 1 day dosing only

Interventions

[14C]-bilastine

Single oral dose of 20 mg \[14C\]-bilastine. 1 capsule. 1 day dosing only

Intervention Type: DRUG

Eligibility Criteria

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.

• Minimum Eligible Age: 30 Years
• Maximum Eligible Age: 60 Years
• Eligible Sex: MALE
• Accepts Healthy Volunteers: Yes

Sponsors

Charles River Clinical Services Edinburgh Ltd and CR Laboratories Preclinical Services Ltd

UNKNOWN

Sponsor Role: collaborator

MDS Pharma Services Switzerland AG

UNKNOWN

Sponsor Role: collaborator

Faes Farma, S.A.

INDUSTRY

Sponsor Role: lead

Responsible Party

Responsibility Role: SPONSOR

Principal Investigators

Stuart J Mair, MD

Role: PRINCIPAL_INVESTIGATOR

Syneos Health

Lindsay McGregor

Role: STUDY_DIRECTOR

Syneos Health

Locations

Charles River Laboratories Clinical Services Ltd, Origo Centre

Riccarton, Edinburgh, United Kingdom

Countries

United Kingdom

References

Lucero ML, Gonzalo A, Mumford R, Betanzos M, Alejandro A. An overview of bilastine metabolism during preclinical investigations. Drug Chem Toxicol. 2012 Jun;35 Suppl 1:18-24. doi: 10.3109/01480545.2012.682651.

Reference Type: BACKGROUND

PMID: 22616812 (View on PubMed)

Lucero ML, Patterson AB. Whole-body tissue distribution of total radioactivity in rats after oral administration of [(1)(4)C]-bilastine. Drug Chem Toxicol. 2012 Jun;35 Suppl 1:1-7. doi: 10.3109/01480545.2012.682650.

Reference Type: BACKGROUND

PMID: 22616810 (View on PubMed)

Other Identifiers

EudraCT Number: 2007-003373-12

Identifier Type: -

Identifier Source: secondary_id

CR Study Number: 186781

Identifier Type: -

Identifier Source: secondary_id

BILA 459-13

Identifier Type: -

Identifier Source: org_study_id