A Study to Assess the Absolute Bioavailability and Pharmacokinetics of Simeprevir (TMC435) Administered as Single Oral Doses of TMC435 and an Intravenous Microdose of [3H]-TMC435 in Healthy Male Patients

NCT ID: NCT01707342

Last Updated: 2014-03-28

Basic Information

• Recruitment Status: COMPLETED
• Clinical Phase: PHASE1
• Total Enrollment: 6 participants
• Study Classification: INTERVENTIONAL
• Study Start Date: 2012-10-31
• Study Completion Date: 2012-11-30

Brief Summary

The purpose of this study is to evaluate the absolute bioavailability and pharmacokinetics (what the body does to the medication) of simeprevir (TMC435) after administration of single oral doses of 50 mg and 150 mg when administered together with a single intravenous (IV) dose of 100 microgram [3H]-TMC435 in healthy male participants.

Detailed Description

This is an open-label (all people know the identity of the intervention), sequential (a single group of participants where study medication is administered in a sequence), single-dose study to assess the absolute bioavailability and pharmacokinetics (what the body does to the medication) of single oral doses of 50 mg and 150 mg simeprevir (TMC435) administered together with an intravenous (IV) microdose of 100 microgram [3H]-TMC435 in healthy male participants. The study consists of 3 phases, screening phase (21 days prior to administration of study medication), treatment phase, and a follow up phase. In the treatment phase, participants will receive 2 treatments, ie, Treatment A: single oral dose of simeprevir (TMC435) 50 mg followed 5 hours later by a single 10 minute IV infusion of [3H]-TMC435 (100 microcurie) 100 microgram; and Treatment B: single oral dose of simeprevir (TMC435) 150 mg followed 5 hours later by a single 10 minute IV infusion of [3H]-TMC435 (100 microcurie) 100 microgram. Treatments will be administered in two consecutive treatment periods, first Treatment A in Period 1, followed by Treatment B in Period 2; separated by a washout period (period when the participant is not receiving any study medication) of 7 to 14 days. The follow up will be for 5 to 7 days after end of Period 2. Blood samples will be collected for full plasma pharmacokinetics evaluations; along with urine and stool samples for analysis of total plasma radioactivity. Safety evaluations for adverse events, clinical laboratory tests, electrocardiogram, vital signs, physical examination, liver volume determination, and specific toxicities will be monitored throughout the study. The total duration of the study will be approximately 42 days.

Conditions

Healthy Male Participants

Study Design

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

Study Groups

Simeprevir (TMC435)

Treatment A: single oral dose of simeprevir (TMC435) 50 mg; and Treatment B: single oral dose of simeprevir (TMC435) 150 mg. A single 10 minute intravenous infusion of \[3H\]-TMC435 (100 microcurie) 100 microgram will be followed 5 hours later after administration of Treatment A and Treatment B in Period 1 and Period 2, respectively.

Group Type: EXPERIMENTAL

Simeprevir (TMC435)

Intervention Type: DRUG

Treatment A: Simeprevir (TMC435) 50 mg; and Treatment B: Simeprevir (TMC435) 150 mg; will be followed 5 hours later by a single 10 minute intravenous infusion of \[3H\]-TMC435 (100 microcurie) 100 microgram in Period 1 and Period 2, respectively.

Interventions

Simeprevir (TMC435)

Treatment A: Simeprevir (TMC435) 50 mg; and Treatment B: Simeprevir (TMC435) 150 mg; will be followed 5 hours later by a single 10 minute intravenous infusion of \[3H\]-TMC435 (100 microcurie) 100 microgram in Period 1 and Period 2, respectively.

Intervention Type: DRUG

Eligibility Criteria

Inclusion Criteria

• Must be healthy on the basis of physical examination, medical history, vital signs, 12-lead electrocardiogram, and clinical laboratory tests performed at screening
• Must be non-smoking for at least 3 months prior to screening

Exclusion Criteria

• History of liver or renal insufficiency
• Have any ferromagnetic medical implants or medical devices that can be de-programmed by strong magnetic fields such as, but not limited to: cardiac pacemakers, implantable cardiac defibrillators, cochlear implants, or insulin pumps
• Had a surgical intervention on brain or eyes or has an intraocular foreign metallic object
• Has a history of anxiety and claustrophobia

• Minimum Eligible Age: 18 Years
• Maximum Eligible Age: 55 Years
• Eligible Sex: MALE
• Accepts Healthy Volunteers: Yes

Sponsors

Janssen R&D Ireland

INDUSTRY

Sponsor Role: lead

Responsible Party

Responsibility Role: SPONSOR

Principal Investigators

Janssen R&D Ireland Clinical Trial

Role: STUDY_DIRECTOR

Janssen R&D Ireland

Locations

Merksem, , Belgium

Countries

Belgium

Other Identifiers

TMC435-TiDP16-C118

Identifier Type: OTHER

Identifier Source: secondary_id

2012-002330-37

Identifier Type: EUDRACT_NUMBER

Identifier Source: secondary_id

CR100901

Identifier Type: -

Identifier Source: org_study_id