Phase 1 Absorption Distribution Metabolism and Excretion of AQX-1125

Aquinox Pharmaceuticals (Canada) Inc.9 enrolled

Overview

This study is conducted to evaluate the absolute bioavailability, metabolism and elimination pathways of AQX-1125 in healthy male and female subjects.

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.

Study Type

INTERVENTIONAL

Allocation

NON_RANDOMIZED

Purpose

BASIC_SCIENCE

Masking

NONE

Enrollment

Conditions

Healthy Volunteer

Interventions

AQX-1125 Oral TabletDRUG

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.

[14C]-AQX-1125 IVDRUG

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.

[14C]-AQX-1125 Oral SolutionDRUG

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.

Eligibility

Sex: ALLMin age: 30 YearsMax age: 65 YearsHealthy volunteers:

Medical Language ↔ Plain English

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)

Locations (1)

Quotient Clinical

Nottingham, United Kingdom

Outcomes

Primary Outcomes

Absolute bioavailability (F) of AQX-1125

Time frame: 0 - 96 hrs

Mass balance recovery of total radioactivity in urine, faeces and all excreta

Measure amount excreted (Ae)

Time frame: 0 -168 hrs

Mass balance recovery of total radioactivity in urine, faeces and all excreta

Measure Ae as a percentage of the administered dose (%Ae)

Time frame: 0 -168 hrs

Mass balance recovery of total radioactivity in urine, faeces and all excreta

Cumulative recovery of Ae (Cum Ae)

Time frame: 0 -168 hrs

Mass balance recovery of total radioactivity in urine, faeces and all excreta

Cum Ae expressed as a percentage of the administered dose (Cum %Ae)

Time frame: 0 -168 hrs

Metabolite profiling and structural identification in plasma, urine and faeces to estimate the routes and rates of elimination of [14-C]-AQX-1125

Time frame: 0 -168 hrs

Measure Ae total radioactivity for urine and faeces

Time frame: 0-168 hrs

Measure %Ae total radioactivity for urine and faeces

Time frame: 0-168 hrs

Measure Cum Ae (total) for urine and faeces

Time frame: 0-168 hrs

Measure Cum% Ae (total) for urine and faeces

Time frame: 0-168 hrs

Data from ClinicalTrials.gov

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Secondary Outcomes

PK parameters of AQX-1125 in plasma following oral administration (Part 1)

Measurement of Cmax

Time frame: 0-96 hrs

PK parameters of AQX-1125 in plasma following oral administration (Part 1)

Measurement of Tmax

Time frame: 0-96 hrs

PK parameters of AQX-1125 in plasma following oral administration (Part 1)

Measurement of Tlag

Time frame: 0-96 hrs

PK parameters of AQX-1125 in plasma following oral administration (Part 1)

Measurement of AUC(0-24)

Time frame: 0-96 hrs

PK parameters of AQX-1125 in plasma following oral administration (Part 1)

Measurement of AUC(0-last)

Time frame: 0-96 hrs

PK parameters of AQX-1125 in plasma following oral administration (Part 1)

Measurement of AUC(0-inf)

Time frame: 0-96 hrs

PK parameters of AQX-1125 in plasma following oral administration (Part 1)

Measurement of AUC%extrap

Time frame: 0-96 hrs

PK parameters of AQX-1125 in plasma following oral administration (Part 1)

Measurement of lambda-z

Time frame: 0-96 hrs

PK parameters of AQX-1125 in plasma following oral administration (Part 1)

Measurement of T1/2

Time frame: 0-96 hrs

PK parameters of AQX-1125 in plasma following oral administration (Part 1)

Measurement of CL/F

Time frame: 0-96 hrs

PK parameters of AQX-1125 in plasma following oral administration (Part 1)

Measurement of Vz/F

Time frame: 0-96 hrs

PK parameters of AQX-1125 in plasma following oral administration (Part 1)

Measurement of MRT

Time frame: 0-96 hrs

PK parameters of AQX-1125 in plasma following IV administration (Part 1)

Measurement of Cmax

Time frame: 0 - 96 hrs

PK parameters of AQX-1125 in plasma following IV administration (Part 1)

Measurement of Tmax

Time frame: 0 - 96 hrs

PK parameters of AQX-1125 in plasma following IV administration (Part 1)

Measurement of Tlag

Time frame: 0 - 96 hrs

PK parameters of AQX-1125 in plasma following IV administration (Part 1)

Measurement of AUC(0-24)

Time frame: 0 - 96 hrs

PK parameters of AQX-1125 in plasma following IV administration (Part 1)

Measurement of AUC(0-last)

Time frame: 0 - 96 hrs

PK parameters of AQX-1125 in plasma following IV administration (Part 1)

Measurement of AUC(0-inf)

Time frame: 0 - 96 hrs

PK parameters of AQX-1125 in plasma following IV administration (Part 1)

Measurement of AUC%extrap

Time frame: 0 - 96 hrs

PK parameters of AQX-1125 in plasma following IV administration (Part 1)

Measurement of lambda-z

Time frame: 0 - 96 hrs

PK parameters of AQX-1125 in plasma following IV administration (Part 1)

Measurement of T1/2

Time frame: 0 - 96 hrs

PK parameters of AQX-1125 in plasma following IV administration (Part 1)

Measurement of CL

Time frame: 0 - 96 hrs

PK parameters of AQX-1125 in plasma following IV administration (Part 1)

Measurement of Vz

Time frame: 0 - 96 hrs

PK parameters of AQX-1125 in plasma following IV administration (Part 1)

Measurement of VSS

Time frame: 0 - 96 hrs

PK parameters of AQX-1125 in plasma following IV administration (Part 1)

Measurement of MRT

Time frame: 0 - 96 hrs

Safety and tolerability assessments based on adverse events, safety laboratory tests, vital signs, physical examinations, ECGs and AEs (Part 1)

Time frame: 0 - 96 hrs