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

• Status: Completed
• Trial end date: 2021-10-29
• Target enrollment: 0
• Participant gender: All

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.

• Phase: Phase 1
• Accepts Healthy Volunteers?: Accepts Healthy Volunteers

Details

• Lead Sponsor: Heptares Therapeutics Limited

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