Phase 1 Absorption Distribution Metabolism and Excretion of AQX-1125
- Conditions
- Healthy Volunteer
- Interventions
- Registration Number
- NCT03185195
- Lead Sponsor
- Aquinox Pharmaceuticals (Canada) Inc.
- Brief Summary
This study is conducted to evaluate the absolute bioavailability, metabolism and elimination pathways of AQX-1125 in healthy male and female subjects.
- Detailed Description
This is a single-centre, open-label, non-randomised, 2-part, sequential dose study in healthy male and female subjects. It is planned to enrol a single cohort of 8 healthy subjects (4 male and 4 female) who will participate in Part 1 and Part 2 of the study.
In Part 1, each subject will receive a single oral dose of AQX-1125 followed by an IV microtracer dose of carbon-14-AQX-1125 (\[14C\]-AQX-1125). In Part 2, each subject will receive a single oral dose of \[14C\]-AQX-1125.
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- All
- Target Recruitment
- 9
- Healthy males
- Healthy females of non-child bearing potential
- BMI 18.0 to 35 kg/m2
- History of any drug or alcohol abuse in the past 2 years
- Regular alcohol consumption in males >21 units per week and females >14 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 had smoked within the last 12 months; this included cigarettes, e-cigarettes and nicotine replacement products. Positive cotinine test result at screening and each admission
- Clinically significant abnormal clinical chemistry, haematology, urinalysis or electrocardiogram (ECG)
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- SEQUENTIAL
- Arm && Interventions
Group Intervention Description [14C]-AQX-1125 IV [14C]-AQX-1125 IV Radiolabelled AQX-1125 - Intravenous [14C]-AQX-1125 Oral Solution [14C]-AQX-1125 Oral Solution Radiolabelled AQX-1125 - Oral Solution AQX-1125 Oral Tablet AQX-1125 Oral Tablet AQX-1125 - Oral Tablet
- Primary Outcome Measures
Name Time Method Mass balance recovery of total radioactivity in urine, faeces and all excreta 0 -168 hrs Cum Ae expressed as a percentage of the administered dose (Cum %Ae)
Measure Cum% Ae (total) for urine and faeces 0-168 hrs Absolute bioavailability (F) of AQX-1125 0 - 96 hrs Metabolite profiling and structural identification in plasma, urine and faeces to estimate the routes and rates of elimination of [14-C]-AQX-1125 0 -168 hrs Measure Ae total radioactivity for urine and faeces 0-168 hrs Measure %Ae total radioactivity for urine and faeces 0-168 hrs Measure Cum Ae (total) for urine and faeces 0-168 hrs Measure PK parameters of total radioactivity in plasma following oral administration 0 -96 hrs Cmax
Measure PK parameters of total radioactivity in plasma following oral administration: 0 -96 hrs MRT
- Secondary Outcome Measures
Name Time Method Safety and tolerability assessments based on adverse events, safety laboratory tests, vital signs, physical examinations, ECGs and AEs (Part 1) 0 - 96 hrs Chemical structure of major metabolites of [14-C]-AQX-1125 0 -168 hrs Major metabolites classified as \>10% of the AUC of total radioactivity in plasma and \>10% dose excreted in urine and faeces following oral administration (Part 2)
PK parameters of AQX-1125 in plasma following IV administration (Part 1) 0 - 96 hrs Measurement of MRT
PK parameters of AQX-1125 in plasma following oral administration (Part 1) 0-96 hrs Measurement of MRT
Measure plasma whole blood concentration ratios for total radioactivity (Part 2) 0 -168 hrs Safety and tolerability assessments based on adverse events, safety laboratory tests, vital signs and ECG (Part 2) 0 -168 hrs PK parameters of AQX-1125 in plasma following oral administration (Part 2) 0 -168 hrs Measurement of MRT
Trial Locations
- Locations (1)
Quotient Clinical
🇬🇧Nottingham, United Kingdom