Clinical trial NCT03185195: Phase 1 Absorption Distribution Metabolism and Excretion of AQX-1125
Official title: An Open-Label,2-Part Sequential Dose Study Designed to Assess the Absolute Bioavailability, Mass Balance Recovery, Metabolite Profile and Identification of Metabolite Structure for [14C]-AQX-1125 in Healthy Subjects
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy Volunteer
Lead sponsor: Aquinox Pharmaceuticals (Canada) Inc.
Sponsor class: INDUSTRY
Collaborators: name: Quotient Clinical
First posted: 2017-06-14
Enrollment: 9
Sex: ALL
Minimum age (years): 30
Maximum age (years): 65
Standard ages: ADULT
OLDER_ADULT
Accepts healthy volunteers: yes
Allocation: NON_RANDOMIZED
Intervention model: SEQUENTIAL
Primary purpose: BASIC_SCIENCE

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.

Eligibility criteria: 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)

Primary outcomes:
measure: Absolute bioavailability (F) of AQX-1125
timeFrame: 0 - 96 hrs
measure: Mass balance recovery of total radioactivity in urine, faeces and all excreta
timeFrame: 0 -168 hrs
measure: Mass balance recovery of total radioactivity in urine, faeces and all excreta
timeFrame: 0 -168 hrs
measure: Mass balance recovery of total radioactivity in urine, faeces and all excreta
timeFrame: 0 -168 hrs
measure: Mass balance recovery of total radioactivity in urine, faeces and all excreta
timeFrame: 0 -168 hrs
measure: Metabolite profiling and structural identification in plasma, urine and faeces to estimate the routes and rates of elimination of [14-C]-AQX-1125
timeFrame: 0 -168 hrs
measure: Measure Ae total radioactivity for urine and faeces
timeFrame: 0-168 hrs
measure: Measure %Ae total radioactivity for urine and faeces
timeFrame: 0-168 hrs
measure: Measure Cum Ae (total) for urine and faeces
timeFrame: 0-168 hrs
measure: Measure Cum% Ae (total) for urine and faeces
timeFrame: 0-168 hrs
measure: Measure PK parameters of total radioactivity in plasma following oral administration
timeFrame: 0 -96 hrs
measure: Measure PK parameters of total radioactivity in plasma following oral administration:
timeFrame: 0 -96 hrs
measure: Measure PK parameters of total radioactivity in plasma following oral administration:
timeFrame: 0 -96 hrs
measure: Measure PK parameters of total radioactivity in plasma following oral administration:
timeFrame: 0 -96 hrs
measure: Measure PK parameters of total radioactivity in plasma following oral administration:
timeFrame: 0 -96 hrs
measure: Measure PK parameters of total radioactivity in plasma following oral administration:
timeFrame: 0 -96 hrs
measure: Measure PK parameters of total radioactivity in plasma following oral administration:
timeFrame: 0 -96 hrs
measure: Measure PK parameters of total radioactivity in plasma following oral administration:
timeFrame: 0 -96 hrs
measure: Measure PK parameters of total radioactivity in plasma following oral administration:
timeFrame: 0 -96 hrs
measure: Measure PK parameters of total radioactivity in plasma following oral administration:
timeFrame: 0 -96 hrs
measure: Measure PK parameters of total radioactivity in plasma following oral administration:
timeFrame: 0 -96 hrs
measure: Measure PK parameters of total radioactivity in plasma following oral administration:
timeFrame: 0 -96 hrs
Secondary outcomes:
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 1)
timeFrame: 0-96 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 1)
timeFrame: 0-96 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 1)
timeFrame: 0-96 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 1)
timeFrame: 0-96 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 1)
timeFrame: 0-96 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 1)
timeFrame: 0-96 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 1)
timeFrame: 0-96 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 1)
timeFrame: 0-96 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 1)
timeFrame: 0-96 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 1)
timeFrame: 0-96 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 1)
timeFrame: 0-96 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 1)
timeFrame: 0-96 hrs
measure: PK parameters of AQX-1125 in plasma following IV administration (Part 1)
timeFrame: 0 - 96 hrs
measure: PK parameters of AQX-1125 in plasma following IV administration (Part 1)
timeFrame: 0 - 96 hrs
measure: PK parameters of AQX-1125 in plasma following IV administration (Part 1)
timeFrame: 0 - 96 hrs
measure: PK parameters of AQX-1125 in plasma following IV administration (Part 1)
timeFrame: 0 - 96 hrs
measure: PK parameters of AQX-1125 in plasma following IV administration (Part 1)
timeFrame: 0 - 96 hrs
measure: PK parameters of AQX-1125 in plasma following IV administration (Part 1)
timeFrame: 0 - 96 hrs
measure: PK parameters of AQX-1125 in plasma following IV administration (Part 1)
timeFrame: 0 - 96 hrs
measure: PK parameters of AQX-1125 in plasma following IV administration (Part 1)
timeFrame: 0 - 96 hrs
measure: PK parameters of AQX-1125 in plasma following IV administration (Part 1)
timeFrame: 0 - 96 hrs
measure: PK parameters of AQX-1125 in plasma following IV administration (Part 1)
timeFrame: 0 - 96 hrs
measure: PK parameters of AQX-1125 in plasma following IV administration (Part 1)
timeFrame: 0 - 96 hrs
measure: PK parameters of AQX-1125 in plasma following IV administration (Part 1)
timeFrame: 0 - 96 hrs
measure: PK parameters of AQX-1125 in plasma following IV administration (Part 1)
timeFrame: 0 - 96 hrs
measure: Safety and tolerability assessments based on adverse events, safety laboratory tests, vital signs, physical examinations, ECGs and AEs (Part 1)
timeFrame: 0 - 96 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 2)
timeFrame: 0 -168 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 2)
timeFrame: 0 -168 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 2)
timeFrame: 0 -168 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 2)
timeFrame: 0 -168 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 2)
timeFrame: 0 -168 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 2)
timeFrame: 0 -168 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 2)
timeFrame: 0 -168 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 2)
timeFrame: 0 -168 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 2)
timeFrame: 0 -168 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 2)
timeFrame: 0 -168 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 2)
timeFrame: 0 -168 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 2)
timeFrame: 0 -168 hrs
measure: PK parameters of AQX-1125 in plasma following oral administration (Part 2)
timeFrame: 0 -168 hrs
measure: Measure plasma whole blood concentration ratios for total radioactivity (Part 2)
timeFrame: 0 -168 hrs
measure: Chemical structure of major metabolites of [14-C]-AQX-1125
timeFrame: 0 -168 hrs
measure: Safety and tolerability assessments based on adverse events, safety laboratory tests, vital signs and ECG (Part 2)
timeFrame: 0 -168 hrs
Other outcomes:
Locations:
city: Nottingham
country: United Kingdom
facility: Quotient Clinical
Study officials:
affiliation: Quotient Clinical
name: Dr.Nand Singh, MD
role: PRINCIPAL_INVESTIGATOR
References: