Working…
ClinicalTrials.gov
ClinicalTrials.gov Menu

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.
 
ClinicalTrials.gov Identifier: NCT04935320
Recruitment Status : Completed
First Posted : June 23, 2021
Last Update Posted : November 2, 2021
Sponsor:
Information provided by (Responsible Party):
Heptares Therapeutics Limited

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.

Condition or disease Intervention/treatment Phase
Healthy Subjects Drug: HTL0016878.HCl Solution 10 mg Drug: HTL0016878.Citrate Capsule 10 mg Phase 1

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.

Layout table for study information
Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 15 participants
Allocation: Randomized
Intervention Model: Crossover Assignment
Masking: None (Open Label)
Primary Purpose: Treatment
Official Title: 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
Actual Study Start Date : July 27, 2021
Actual Primary Completion Date : October 29, 2021
Actual Study Completion Date : October 29, 2021

Arm Intervention/treatment
Experimental: Oral Solution Fasted
HTL0016878.HCl 10 mg, single dose, oral solution, fasted
Drug: HTL0016878.HCl Solution 10 mg
Oral solution fasted

Experimental: Oral Capsule Fasted
HTL0016878.citrate 10 mg, single dose, oral capsule, fasted
Drug: HTL0016878.Citrate Capsule 10 mg
Oral capsule fed or fasted

Experimental: Oral Capsule Fed
HTL0016878.citrate 10 mg, single dose, oral capsule, fed
Drug: HTL0016878.Citrate Capsule 10 mg
Oral capsule fed or fasted




Primary Outcome Measures :
  1. Concentration of HTL0016878 in plasma Cmax [ Time Frame: 0-72 hours ]
    Pharmacokinetics

  2. Concentration of HTL0016878 in plasma AUC [ Time Frame: 0-72 hours ]
    Pharmacokinetics


Secondary Outcome Measures :
  1. Treatment Emergent Adverse Events [ Time Frame: Baseline up to 13 days post-dose ]
    Safety and Tolerability



Information from the National Library of Medicine

Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the contacts provided below. For general information, Learn About Clinical Studies.


Layout table for eligibility information
Ages Eligible for Study:   18 Years to 50 Years   (Adult)
Sexes Eligible for Study:   All
Accepts Healthy Volunteers:   Yes
Criteria

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

Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT04935320


Locations
Layout table for location information
United Kingdom
Hammersmith Medicines Research Ltd (HMR)
London, United Kingdom, NW10 7EW
Sponsors and Collaborators
Heptares Therapeutics Limited
Layout table for additonal information
Responsible Party: Heptares Therapeutics Limited
ClinicalTrials.gov Identifier: NCT04935320    
Other Study ID Numbers: HTL0016878-102
18-018 ( Other Identifier: Hammersmith Medicines Research Ltd )
2018-003685-14 ( EudraCT Number )
First Posted: June 23, 2021    Key Record Dates
Last Update Posted: November 2, 2021
Last Verified: November 2021
Individual Participant Data (IPD) Sharing Statement:
Plan to Share IPD: No

Layout table for additional information
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
Keywords provided by Heptares Therapeutics Limited:
Relative Bioavailability