Human Mass Balance Study With Bilastine

A Phase I Study to Investigate the Absorption, Metabolism and Excretion of [14C]-Bilastine Following Oral Administration to Healthy Volunteers

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

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: [14C]-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.

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Contacts and Locations

Study Locations

• United Kingdom
  • Edinburgh
    • Riccarton, Edinburgh, United Kingdom, EH14 4AP
      • Charles River Laboratories Clinical Services Ltd, Origo Centre

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 30 years to 60 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: Male

Description

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.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: I; Single oral dose of 20 mg [14C]-bilastine	Drug: [14C]-bilastine; Single oral dose of 20 mg [14C]-bilastine. 1 capsule. 1 day dosing only

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
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

Collaborators and Investigators

• Sponsor: Faes Farma, S.A.
• Collaborators: Charles River Clinical Services Edinburgh Ltd and CR Laboratories Preclinical Services Ltd; MDS Pharma Services Switzerland AG
• Investigators: Principal Investigator: Stuart J Mair, MD, Syneos Health; Study Director: Lindsay McGregor, Syneos Health

Publications and helpful links

General Publications

• 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. Erratum In: Drug Chem Toxicol. 2012 Oct;35(4):472.
• 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. Erratum In: Drug Chem Toxicol. 2012 Oct;35(4):472.

Study record dates

Study Major Dates

• Study Start: November 1, 2007
• Primary Completion (Actual): December 1, 2007
• Study Completion (Actual): December 1, 2007

Study Registration Dates

• First Submitted: December 12, 2007
• First Submitted That Met QC Criteria: December 12, 2007
• First Posted (Estimate): December 13, 2007

Study Record Updates

• Last Update Posted (Estimate): September 26, 2012
• Last Update Submitted That Met QC Criteria: September 25, 2012
• Last Verified: September 1, 2012

More Information

Terms related to this study

• Keywords: Pharmacokinetics; Absorption; Metabolism; Excretion; Mass Balance
• Other Study ID Numbers: BILA 459-13; EudraCT Number: 2007-003373-12; CR Study Number: 186781