Healthy Volunteer
Conditions
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.
Interventions
DRUGAQX-1125 Oral Tablet
Part 1: Subjects will receive a single oral dose of AQX-1125 followed by \[14C\]-AQX-1125 IV Microtracer dose. In Part 2 subjects receive \[14C\]-AQX-1125 oral solution.
DRUG[14C]-AQX-1125 IV
Part 1: Subjects will receive a single oral dose of AQX-1125 followed by \[14C\]-AQX-1125 IV Microtracer dose. In Part 2 subjects receive \[14C\]-AQX-1125 oral solution.
DRUG[14C]-AQX-1125 Oral Solution
Part 1: Subjects will receive a single oral dose of AQX-1125 followed by \[14C\]-AQX-1125 IV Microtracer dose. In Part 2 subjects receive \[14C\]-AQX-1125 oral solution.
Sponsors
Quotient Clinical
Aquinox Pharmaceuticals (Canada) Inc.
Study design
Allocation
NON_RANDOMIZED
Intervention model
SEQUENTIAL
Primary purpose
BASIC_SCIENCE
Masking
NONE
Masking description
Open-Label
Eligibility
Sex/Gender
ALL
Age
30 Years to 65 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy males * Healthy females of non-child bearing potential * BMI 18.0 to 35 kg/m2
Exclusion criteria
* 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)
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Measure PK parameters of total radioactivity in plasma following oral administration: | 0 -96 hrs | Tmax |
| Mass balance recovery of total radioactivity in urine, faeces and all excreta | 0 -168 hrs | Measure amount excreted (Ae) |
| 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 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 |
| Absolute bioavailability (F) of AQX-1125 | 0 - 96 hrs | — |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| PK parameters of AQX-1125 in plasma following IV administration (Part 1) | 0 - 96 hrs | Measurement of Cmax |
| Safety and tolerability assessments based on adverse events, safety laboratory tests, vital signs, physical examinations, ECGs and AEs (Part 1) | 0 - 96 hrs | — |
| PK parameters of AQX-1125 in plasma following oral administration (Part 2) | 0 -168 hrs | Measurement of Cmax |
| Measure plasma whole blood concentration ratios for total radioactivity (Part 2) | 0 -168 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) |
| 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 1) | 0-96 hrs | Measurement of Cmax |
Countries
United Kingdom
Outcome results
None listed