Human Mass Balance Study With Bilastine

NCT00572611 | Completed Phase 1

• 3 other identifiers: BILA 459-13EudraCT Number: 2007-003373-12CR Study Number: 186781
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

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

Conditions

Healthy

Keywords

Mass Balance; Metabolism; Absorption; Excretion; Pharmacokinetics

Outcome Measures

Primary Outcomes (3)

• Whole blood and plasma concentrations of total radioactivity and parent drug

  168-216 h after dosing, depending on the radioactivity recovery

• Urine and faecal recovery of total radioactivity

  168-216 h after dosing, depending on the radioactivity recovery

• Characterisation and identification of metabolites in plasma, urine and faeces

  168-216 h after dosing, depending on the radioactivity recovery

Study Arms (1)

I

EXPERIMENTAL

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

Drug: [14C]-bilastine

Interventions

[14C]-bilastine DRUG

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

I

Eligibility Criteria

• Age: 30 Years - 60 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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.

You may not qualify if:

• 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.

Sponsors & Collaborators

• Faes Farma, S.A.: lead
• Charles River Clinical Services Edinburgh Ltd and CR Laboratories Preclinical Services Ltd: collaborator
• MDS Pharma Services Switzerland AG: collaborator

Study Sites (1)

Charles River Laboratories Clinical Services Ltd, Origo Centre

Riccarton, Edinburgh, EH14 4AP, United Kingdom

Location

Related Publications (2)

• 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.

  PMID: 22616812 BACKGROUND

• 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.

  PMID: 22616810 BACKGROUND

Study Officials

• Stuart J Mair, MD

  Syneos Health

  PRINCIPAL INVESTIGATOR

• Lindsay McGregor

  Syneos Health

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: December 12, 2007
• First Posted: December 13, 2007
• Study Start: November 1, 2007
• Primary Completion: December 1, 2007
• Study Completion: December 1, 2007
• Last Updated: September 26, 2012

Record last verified: 2012-09

Locations

GB (1)