Absorption, Metabolism and Excretion Study of [14C]PBT2 and Absolute Bioavailability of PBT2

Phase 1

Completed

• Conditions: Healthy Volunteers
• Interventions: Drug: oral 14C-PBT2; Drug: IV PBT2 microtracer and oral PBT2 single dose

• Registration Number: NCT02249728
• Lead Sponsor: Prana Biotechnology Limited

Brief Summary

The purpose of the study is to investigate how the test drug, PBT2, is taken up, broken down and removed from the body when given as an oral capsule, a radiolabelled oral suspension and a radiolabelled intravenous injection.

Detailed Description

Not available

Study Timeline

• Study Start: 2014-06
• Primary Completion: 2014-07
• Study Completion: 2014-07
• Study First Submitted: 2014-07-30
• Study First Submitted QC: 2014-09-25
• Study First Posted: 2014-09-26
• Results First Submitted: 2015-11-17
• Status Verified: 2016-02
• Results First Submitted QC: 2016-02-28
• Last Update Submitted: 2016-02-28
• Results First Posted: 2016-03-30
• Last Update Posted: 2016-03-30

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 6

Inclusion Criteria

• Healthy males
• Body mass index of 18.0 to 35.0 kg/m2

Exclusion Criteria

• History of any drug or alcohol abuse in the past 2 years
• Regular alcohol consumption >21 units per week (1 unit = ½ pint beer, 25 mL of 40% spirit or a 125 mL glass of wine)
• Current smokers and those who have smoked within the last 12 months
• Radiation exposure, including that from the present study, excluding background radiation but including diagnostic x-rays and other medical exposures, exceeding 5 mSv in the last 12 months or 10 mSv in the last 5 years.
• Clinically significant abnormal biochemistry, haematology or urinalysis as judged by the investigator
• Positive drugs of abuse test result
• Positive hepatitis B surface antigen (HBsAg), hepatitis C virus antibody (HCV Ab) or human immunodeficiency virus (HIV) results
• History of cardiovascular, renal, hepatic, chronic respiratory or GI disease as judged by the investigator

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: SINGLE_GROUP

Arm && Interventions

Group	Intervention	Description
Radiolabelled AME	oral 14C-PBT2	oral 14C PBT2
Absolute Bioavailability	IV PBT2 microtracer and oral PBT2 single dose	IV PBT2 microtracer and oral PBT2 single dose

Primary Outcome Measures

Name	Time	Method
Mass Balance	168 h (7 days) post dose	Amount excreted as a percentage of the administered dose (%Ae)
Absolute Bioavailability of PBT2 (F%)	0 to 72 hours post oral dose	Absolute bioavailability is the amount of drug from a formulation that reaches the systemic circulation relative to an IV dose, computed as AUC(oral)/AUC(IV), with range from 0% (no drug) to 100% (all of the administered drug).

Secondary Outcome Measures

Name	Time	Method
Oral PK Profile of PBT2 as Assessed by AUC(0-last)	72 h post oral dose	Area under the plasma concentration vs time curve from time 0h to the last time point of oral PBT2 .
Ratio of Whole Blood, Plasma [14C] PBT2 at 24 Hours	0 to 24 hours	Ratio of whole blood, plasma \[14C\] PBT2 at 24 hours
Oral PK Profile of [14C]-PBT2 as Assessed by AUC(0-last)	0 to 72 hours	area under the plasma concentration vs time curve to the last timepoint
IV PK Profile of [14C]-PBT2 and Total Radioactivity as Assessed by AUC(0 Last)	0 to 72 h post oral dose	Area under the plasma concentration vs time curve from time 0h to the last time point of IV \[14C\]-PBT2 .
Safety and Tolerability of PBT2	72 h post oral dose	As assessed by the number of participants with adverse events

Trial Locations

Locations (1)

Quotient Clinical; 🇬🇧 Nottingham, Nottinghamshire, United Kingdom