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Completed

NCT Number: NCT02710188

Relative Bioavailability Study in Healthy Subjects to Evaluate the Pharmacokinetics of HTL0009936 After One Dose of Prototype Formulation

The purpose of this study is to find a modified release oral tablet formulation for this drug, which will be safe and well tolerated.

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Key information

Conditions

Alzheimer's Disease Alzheimer Disease Brain Diseases Central Nervous System Diseases Dementia Mental Disorders Nervous System Diseases Neurocognitive Disorders Neurodegenerative Diseases Tauopathies

Age range

18 year–65 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

Quotient Clinical

Ruddington, Nottingham, NG11 6JS, United Kingdom

About this study

The aim of the study is to develop a modified release oral tablet formulation that maintains plasma concentrations within the target therapeutic range, and is safe and tolerable.

Who can participate

Healthy volunteers accepted: Yes

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

Inclusion criteria

  • Healthy males & females
  • Aged 18 to 65 years
  • Body mass index of 18.0 to 35.0 kg/m2
  • CYP2D6 (intermediate or extensive metabolizer)

Exclusion criteria

  • Subjects with a resting heart rate (HR) >90 bpm, and/or systolic blood pressure (BP) >150 mmHg, and/or diastolic BP >90 mmHg
  • Subjects with QT interval corrected for heart rate using Fridericia's formula (QTcF) >450 ms (males) or >470 ms (females)
  • Personal or family history of long QT syndrome or sudden death
  • Subjects who are CYP2D6 (poor or ultra-rapid metabolizer)

Treatment and study plan

HTL0009936 modified release

Drug

HTL0009936 modified release

HTL0009936 immediate release

Drug

HTL0009936 immediate release

Primary outcomes

  1. Tlag

    Time frame: 14 weeks

    The PK profiles of HTL0009936 Modified release oral prototype formulations in healthy CYP2D6 IM and EM subjects. Calculation of the elapsed time from dosing at which HTL0009936 was first quantifiable in a concentration vs time profile (Tlag).

  2. Frel

    Time frame: 14 weeks

    The PK profiles of HTL0009936 Modified release oral prototype formulations in healthy CYP2D6 IM and EM subjects. Calculation of relative bioavailability (Frel) of HTL0009936 MR prototype formulations compared to the IR reference formulation and, if applicable, MR prototype formulations in the fed state compared to fasted state.

  3. Tmax

    Time frame: 14 weeks

    The PK profiles of HTL0009936 Modified release oral prototype formulations in healthy CYP2D6 IM and EM subjects. Calculation of the elapsed time from dosing at which the maximum observed HTL0009936 concentration (Cmax) was apparent (Tmax)

  4. Cmax

    Time frame: 14 weeks

    The PK profiles of HTL0009936 Modified release oral prototype formulations in healthy CYP2D6 IM and EM subjects. Calculation of Cmax.

  5. Concentration of HTL0009936 at 6 hours post dose (C6)

    Time frame: 6 hours post dose

    The PK profiles of HTL0009936 Modified release oral prototype formulations in healthy CYP2D6 IM and EM subjects. Calculation of HTL0009936 concentration at 6 hours post-dose (C6)

  6. AUC (0-last)

    Time frame: 14 weeks

    The PK profiles of HTL0009936 Modified release oral prototype formulations in healthy CYP2D6 IM and EM subjects. Calculation of the area under the concentration versus time curve from time zero to the last measurable concentration (AUC(0-last))

  7. AUC (0-inf)

    Time frame: 14 weeks

    The PK profiles of HTL0009936 Modified release oral prototype formulations in healthy CYP2D6 IM and EM subjects. Calculation of the area under the concentration versus time curve from time zero to extrapolated to infinity (AUC(0-inf)).

  8. AUC%extrap

    Time frame: 14 weeks

    The PK profiles of HTL0009936 Modified release oral prototype formulations in healthy CYP2D6 IM and EM subjects. Calculation of percentage of AUC(0-inf) extrapolated beyond last measured time point (AUC%extrap).

  9. Lambda-z

    Time frame: 14 weeks

    The PK profiles of HTL0009936 Modified release oral prototype formulations in healthy CYP2D6 IM and EM subjects. Calculation of the slope of the apparent elimination phase (Lambda-z).

  10. T1/2

    Time frame: 14 weeks

    The PK profiles of HTL0009936 Modified release oral prototype formulations in healthy CYP2D6 IM and EM subjects. Calculation of the apparent elimination half-life (T1/2).

  11. Dose normalized AUC

    Time frame: 14 weeks

    The PK profiles of HTL0009936 Modified release oral prototype formulations in healthy CYP2D6 IM and EM subjects. In addition, if different dose levels of the same prototype are administered, dose normalized AUC (AUC/D) will be calculated.

  12. Dose normalized Cmax

    Time frame: 14 weeks

    The PK profiles of HTL0009936 Modified release oral prototype formulations in healthy CYP2D6 IM and EM subjects. In addition, if different dose levels of the same prototype are administered, dose normalized Cmax (Cmax/D) will be calculated.

  13. Concentration of HTL0009936 at 12 hours post dose (C12)

    Time frame: 12 hours post dose

    The PK profiles of HTL0009936 Modified release oral prototype formulations in healthy CYP2D6 IM and EM subjects. Calculation of HTL0009936 concentration at 12 hours post-dose (C12)

  14. Concentration of HTL0009936 at 24 hours post dose (C24)

    Time frame: 24 hours post dose

    The PK profiles of HTL0009936 Modified release oral prototype formulations in healthy CYP2D6 IM and EM subjects. Calculation of HTL0009936 concentration at 24 hours post-dose (C24)

Sponsors and collaborators

Lead sponsor

Nxera Pharma UK Limited

Industry

Collaborators

  • Quotient Clinical

Registry information

Official study title

A Phase 1 Relative Bioavailability Study in Healthy CYP2D6 Intermediate (IM) and Extensive Metaboliser (EM) Subjects, Designed to Evaluate the Pharmacokinetic (PK) Profile of HTL0009936 Following Single Dose Administration of Modified Release (MR) Prototype Formulations

Important dates

Study start
2016
Primary completion
2016
Study completion
2016
First posted
Mar 16, 2016
Registry last updated
Oct 18, 2016

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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