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Comparison of Blood Levels of HTL0016878 From an Oral Capsule and an Oral Solution

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details. Identifier: NCT04935320
Recruitment Status : Completed
First Posted : June 23, 2021
Last Update Posted : November 2, 2021
Information provided by (Responsible Party):
Heptares Therapeutics Limited

Tracking Information
First Submitted Date  ICMJE June 21, 2021
First Posted Date  ICMJE June 23, 2021
Last Update Posted Date November 2, 2021
Actual Study Start Date  ICMJE July 27, 2021
Actual Primary Completion Date October 29, 2021   (Final data collection date for primary outcome measure)
Current Primary Outcome Measures  ICMJE
 (submitted: June 21, 2021)
  • Concentration of HTL0016878 in plasma Cmax [ Time Frame: 0-72 hours ]
  • Concentration of HTL0016878 in plasma AUC [ Time Frame: 0-72 hours ]
Original Primary Outcome Measures  ICMJE Same as current
Change History
Current Secondary Outcome Measures  ICMJE
 (submitted: June 21, 2021)
Treatment Emergent Adverse Events [ Time Frame: Baseline up to 13 days post-dose ]
Safety and Tolerability
Original Secondary Outcome Measures  ICMJE Same as current
Current Other Pre-specified Outcome Measures Not Provided
Original Other Pre-specified Outcome Measures Not Provided
Descriptive Information
Brief Title  ICMJE Comparison of Blood Levels of HTL0016878 From an Oral Capsule and an Oral Solution
Official Title  ICMJE Phase 1, Randomised, Open-label, 3-period Crossover, Single Dose Study in Healthy Subjects, to Assess Relative Bioavailability From an Oral Capsule of HTL0016878 Citrate Salt Versus an Oral Solution of HTL0016878 Hydrochloride Salt
Brief Summary This is a randomised, open-label, 3-period, crossover single dose study to assess the relative bioavailability of two formulations of HTL0016878: an oral solution of HCl salt form (the reference product) and an oral capsule containing citrate salt (the test product); and of the effect of food on the pharmacokinetics of the capsule formulation.
Detailed Description Fifteen healthy male or female subjects will be enrolled. Each subject will have 3 study sessions and receive a single oral dose of 10 mg HTL0016878 on Day 1 of each study session. Subjects will receive the HTL0016878.HCl oral solution in the fasted state in 1 session, and the HTL0016878.citrate capsule, in the fasted state and after a high-fat meal, respectively, in the other 2 sessions. Each subject will be randomised to 1 of 3 treatment sequences (5 subjects to each sequence). There will be a washout of at least 10 days between doses. Subjects will be screened within 35 days before their first dose of HTL0016878. In each study session, subjects will be resident on the ward from the day before dosing (Day -1) until completion of procedures 72 h after their dose (Day 4). Subjects will return for a follow up visit 10-13 days after their final dose of trial medication.
Study Type  ICMJE Interventional
Study Phase  ICMJE Phase 1
Study Design  ICMJE Allocation: Randomized
Intervention Model: Crossover Assignment
Masking: None (Open Label)
Primary Purpose: Treatment
Condition  ICMJE Healthy Subjects
Intervention  ICMJE
  • Drug: HTL0016878.HCl Solution 10 mg
    Oral solution fasted
  • Drug: HTL0016878.Citrate Capsule 10 mg
    Oral capsule fed or fasted
Study Arms  ICMJE
  • Experimental: Oral Solution Fasted
    HTL0016878.HCl 10 mg, single dose, oral solution, fasted
    Intervention: Drug: HTL0016878.HCl Solution 10 mg
  • Experimental: Oral Capsule Fasted
    HTL0016878.citrate 10 mg, single dose, oral capsule, fasted
    Intervention: Drug: HTL0016878.Citrate Capsule 10 mg
  • Experimental: Oral Capsule Fed
    HTL0016878.citrate 10 mg, single dose, oral capsule, fed
    Intervention: Drug: HTL0016878.Citrate Capsule 10 mg
Publications * Not Provided

*   Includes publications given by the data provider as well as publications identified by Identifier (NCT Number) in Medline.
Recruitment Information
Recruitment Status  ICMJE Completed
Actual Enrollment  ICMJE
 (submitted: June 21, 2021)
Original Estimated Enrollment  ICMJE Same as current
Actual Study Completion Date  ICMJE October 29, 2021
Actual Primary Completion Date October 29, 2021   (Final data collection date for primary outcome measure)
Eligibility Criteria  ICMJE

Inclusion Criteria:

  1. Healthy male or females, aged 18-50 years
  2. Female subjects must agree to use highly effective contraception
  3. Weigh 60 kg or more, with a BMI in the range 18.0-30.0 kg/m2
  4. Sufficient intelligence to understand the nature of the trial
  5. Willingness to give written consent to participate
  6. Agree to use the contraception requirements of the trial
  7. Agree not to donate blood or blood products during the study and for up to 3 months after the administration of the trial medication
  8. Willingness to give written consent to have data entered into The Overvolunteering Prevention System

Exclusion Criteria:

  1. Woman who is pregnant or lactating
  2. Clinically relevant abnormal history, physical findings, ECG, or laboratory values
  3. Presence or history of acute or chronic illness, or mental health problem
  4. Impaired neurological, endocrine, thyroid, cardiovascular, respiratory, gastrointestinal, hepatic or renal function, diabetes mellitus, coronary heart disease, or history of any psychiatric disorder or psychotic mental illness
  5. Cancer during the 5 years before screening
  6. Supine blood pressure and heart rate outside the ranges: 90-140 mm Hg systolic and 50-90 mm Hg diastolic blood pressure; heart rate 45-80 beats/min
  7. Supine QT interval (QTcF) outside the ranges 300-450 msec (men) and 300-470 msec (women)
  8. Personal or family history of long QT syndrome or family sudden death
  9. Positive test for hepatitis B, hepatitis C or HIV
  10. Aspartate aminotransferase, alanine aminotransferase, gamma glutamyl transferase or total bilirubin levels > 1.5 times the upper limit of normal
  11. Creatinine clearance < 80 mL/min/1.73 m2
  12. Presence or history of drug or alcohol abuse in the past 5 years; or regular intake of more than 21 units of alcohol weekly (for men) or 14 units of alcohol weekly (for women); or use of cigarettes, tobacco and/or nicotine-containing products during the 3 months before dosing
  13. Evidence of drug abuse or positive alcohol or cotinine test results
  14. Positive pregnancy test
  15. Habitual and heavy consumption of caffeinated beverages
  16. Use of a prescription or over-the-counter medicine, any herbal remedy, or nutritional supplement
  17. Receipt of a vaccine against COVID-19 in the 14 days before dosing
  18. Received live attenuated vaccination within 6 weeks prior to Screening
  19. History of severe allergies
  20. Use of any drugs that are inhibitors of CYP2D6
  21. Poor metaboliser of CYP2D6
  22. History of epilepsy or seizures
  23. Any disease associated with cognitive impairment and/or psychosis
  24. Suicidal thoughts or ideation, or insomnia
  25. Any history of mental illness (including anxiety, depression), which required medical intervention
  26. Presence or history of severe adverse reaction to any drug
  27. Surgery or medical condition that might affect absorption of medicines
  28. Receipt of an investigational product as part of another clinical trial within the 3 months before dosing in this study
  29. Receipt of HTL0016878 in a previous clinical trial
  30. Loss of more than 400 mL blood during the 3 months before dosing
  31. Unwilling to eat a high-fat breakfast
  32. Possibility that the volunteer will not cooperate with the requirements of the protocol
  33. Objection by GP to volunteer entering trial
Sex/Gender  ICMJE
Sexes Eligible for Study: All
Ages  ICMJE 18 Years to 50 Years   (Adult)
Accepts Healthy Volunteers  ICMJE Yes
Contacts  ICMJE Contact information is only displayed when the study is recruiting subjects
Listed Location Countries  ICMJE United Kingdom
Removed Location Countries  
Administrative Information
NCT Number  ICMJE NCT04935320
Other Study ID Numbers  ICMJE HTL0016878-102
18-018 ( Other Identifier: Hammersmith Medicines Research Ltd )
2018-003685-14 ( EudraCT Number )
Has Data Monitoring Committee No
U.S. FDA-regulated Product
Studies a U.S. FDA-regulated Drug Product: No
Studies a U.S. FDA-regulated Device Product: No
Product Manufactured in and Exported from the U.S.: No
IPD Sharing Statement  ICMJE
Plan to Share IPD: No
Responsible Party Heptares Therapeutics Limited
Study Sponsor  ICMJE Heptares Therapeutics Limited
Collaborators  ICMJE Not Provided
Investigators  ICMJE Not Provided
PRS Account Heptares Therapeutics Limited
Verification Date November 2021

ICMJE     Data element required by the International Committee of Medical Journal Editors and the World Health Organization ICTRP