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Completed

NCT Number: NCT03185195

Phase 1 Absorption Distribution Metabolism and Excretion of AQX-1125

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

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Key information

Conditions

Healthy Volunteer

Age range

30 year–65 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

Quotient Clinical

Nottingham, United Kingdom

About this study

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.

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

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)

Treatment and study plan

AQX-1125 Oral Tablet

Drug

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 IV

Drug

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.

Other names: Radiolabelled AQX-1125 IV

[14C]-AQX-1125 Oral Solution

Drug

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.

Other names: Radiolabelled AQX-1125 Oral Solution

Primary outcomes

  1. Absolute bioavailability (F) of AQX-1125

    Time frame: 0 - 96 hrs

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

    Time frame: 0 -168 hrs

    Measure amount excreted (Ae)

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

    Time frame: 0 -168 hrs

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

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

    Time frame: 0 -168 hrs

    Cumulative recovery of Ae (Cum Ae)

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

    Time frame: 0 -168 hrs

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

  6. 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

  7. Measure Ae total radioactivity for urine and faeces

    Time frame: 0-168 hrs

  8. Measure %Ae total radioactivity for urine and faeces

    Time frame: 0-168 hrs

  9. Measure Cum Ae (total) for urine and faeces

    Time frame: 0-168 hrs

  10. Measure Cum% Ae (total) for urine and faeces

    Time frame: 0-168 hrs

  11. Measure PK parameters of total radioactivity in plasma following oral administration

    Time frame: 0 -96 hrs

    Cmax

  12. Measure PK parameters of total radioactivity in plasma following oral administration:

    Time frame: 0 -96 hrs

    Tmax

  13. Measure PK parameters of total radioactivity in plasma following oral administration:

    Time frame: 0 -96 hrs

    Tlag

  14. Measure PK parameters of total radioactivity in plasma following oral administration:

    Time frame: 0 -96 hrs

    AUC (0-24)

  15. Measure PK parameters of total radioactivity in plasma following oral administration:

    Time frame: 0 -96 hrs

    AUC (0-last)

  16. Measure PK parameters of total radioactivity in plasma following oral administration:

    Time frame: 0 -96 hrs

    AUC (0-inf)

  17. Measure PK parameters of total radioactivity in plasma following oral administration:

    Time frame: 0 -96 hrs

    AUC % extrap

  18. Measure PK parameters of total radioactivity in plasma following oral administration:

    Time frame: 0 -96 hrs

    lambda-z

  19. Measure PK parameters of total radioactivity in plasma following oral administration:

    Time frame: 0 -96 hrs

    T1/2

  20. Measure PK parameters of total radioactivity in plasma following oral administration:

    Time frame: 0 -96 hrs

    CL/F

  21. Measure PK parameters of total radioactivity in plasma following oral administration:

    Time frame: 0 -96 hrs

    Vz/F

  22. Measure PK parameters of total radioactivity in plasma following oral administration:

    Time frame: 0 -96 hrs

    MRT

Secondary outcomes

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

    Time frame: 0-96 hrs

    Measurement of Cmax

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

    Time frame: 0-96 hrs

    Measurement of Tmax

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

    Time frame: 0-96 hrs

    Measurement of Tlag

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

    Time frame: 0-96 hrs

    Measurement of AUC(0-24)

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

    Time frame: 0-96 hrs

    Measurement of AUC(0-last)

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

    Time frame: 0-96 hrs

    Measurement of AUC(0-inf)

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

    Time frame: 0-96 hrs

    Measurement of AUC%extrap

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

    Time frame: 0-96 hrs

    Measurement of lambda-z

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

    Time frame: 0-96 hrs

    Measurement of T1/2

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

    Time frame: 0-96 hrs

    Measurement of CL/F

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

    Time frame: 0-96 hrs

    Measurement of Vz/F

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

    Time frame: 0-96 hrs

    Measurement of MRT

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

    Time frame: 0 - 96 hrs

    Measurement of Cmax

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

    Time frame: 0 - 96 hrs

    Measurement of Tmax

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

    Time frame: 0 - 96 hrs

    Measurement of Tlag

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

    Time frame: 0 - 96 hrs

    Measurement of AUC(0-24)

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

    Time frame: 0 - 96 hrs

    Measurement of AUC(0-last)

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

    Time frame: 0 - 96 hrs

    Measurement of AUC(0-inf)

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

    Time frame: 0 - 96 hrs

    Measurement of AUC%extrap

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

    Time frame: 0 - 96 hrs

    Measurement of lambda-z

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

    Time frame: 0 - 96 hrs

    Measurement of T1/2

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

    Time frame: 0 - 96 hrs

    Measurement of CL

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

    Time frame: 0 - 96 hrs

    Measurement of Vz

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

    Time frame: 0 - 96 hrs

    Measurement of VSS

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

    Time frame: 0 - 96 hrs

    Measurement of MRT

  26. 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

  27. PK parameters of AQX-1125 in plasma following oral administration (Part 2)

    Time frame: 0 -168 hrs

    Measurement of Cmax

  28. PK parameters of AQX-1125 in plasma following oral administration (Part 2)

    Time frame: 0 -168 hrs

    Measurement of Tmax

  29. PK parameters of AQX-1125 in plasma following oral administration (Part 2)

    Time frame: 0 -168 hrs

    Measurement of Tlag

  30. PK parameters of AQX-1125 in plasma following oral administration (Part 2)

    Time frame: 0 -168 hrs

    Measurement of AUC(0-24)

  31. PK parameters of AQX-1125 in plasma following oral administration (Part 2)

    Time frame: 0 -168 hrs

    Measurement of AUC(0-last)

  32. PK parameters of AQX-1125 in plasma following oral administration (Part 2)

    Time frame: 0 -168 hrs

    Measurement of AUC(0-inf)

  33. PK parameters of AQX-1125 in plasma following oral administration (Part 2)

    Time frame: 0 -168 hrs

    Measurement of AUC%extrap

  34. PK parameters of AQX-1125 in plasma following oral administration (Part 2)

    Time frame: 0 -168 hrs

    Measurement of lambda-z

  35. PK parameters of AQX-1125 in plasma following oral administration (Part 2)

    Time frame: 0 -168 hrs

    Measurement of T1/2

  36. PK parameters of AQX-1125 in plasma following oral administration (Part 2)

    Time frame: 0 -168 hrs

    Measurement of CL/F

  37. PK parameters of AQX-1125 in plasma following oral administration (Part 2)

    Time frame: 0 -168 hrs

    Measurement of Vz/F

  38. PK parameters of AQX-1125 in plasma following oral administration (Part 2)

    Time frame: 0 -168 hrs

    Measurement of F

  39. PK parameters of AQX-1125 in plasma following oral administration (Part 2)

    Time frame: 0 -168 hrs

    Measurement of MRT

  40. Measure plasma whole blood concentration ratios for total radioactivity (Part 2)

    Time frame: 0 -168 hrs

  41. Chemical structure of major metabolites of [14-C]-AQX-1125

    Time frame: 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)

  42. Safety and tolerability assessments based on adverse events, safety laboratory tests, vital signs and ECG (Part 2)

    Time frame: 0 -168 hrs

Sponsors and collaborators

Lead sponsor

Aquinox Pharmaceuticals (Canada) Inc.

Industry

Collaborators

  • Quotient Clinical

Registry information

Official study 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

Acronym: ADME

Important dates

Study start
2016
Primary completion
2017
Study completion
2017
First posted
Jun 14, 2017
Registry last updated
Jun 14, 2017

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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