Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of ACT-451840 in Healthy Subjects (Part A)
Status and phase
Completed
Phase 1
Conditions
Healthy
Treatments
Drug: ACT-451840 200 mg
Drug: ACT-451840 10 mg
Drug: ACT-451840 50 mg
Drug: ACT-451840 (Dose to be determined)
Drug: ACT-451840 500 mg
Drug: ACT-451840 1000 mg
Drug: Placebo
Details and patient eligibility
About
The primary objective of the study was to evaluate the safety and tolerability of ACT-451840 in healthy male subjects.Secondary objectives were : to investigate the pharmacokinetics (PK) of ACT-451840; to investigate the effect of food on the PK of ACT-451840; to evaluate the urinary excretion of ACT-451840 and to investigate the antimalarial activity of ACT-451840.
Enrollment
40 patients
Sex
Male
Ages
18 to 45 years old
Volunteers
Accepts Healthy Volunteers
Inclusion criteria
- Signed informed consent in the local language prior to any study-mandated procedure.
- Body mass index (BMI) of 18.0 to 28.0 kg/m2 (inclusive) at screening.
- Systolic blood pressure 100-145 mmHg, diastolic blood pressure 50-90 mmHg, and pulse rate 45-90 beats per minute (inclusive), measured on the dominant arm, after 5 min in the supine position at screening.
- 12-lead electrocardiogram without clinically relevant abnormalities, measured after 5 min in the supine position at screening.
- Hematology, coagulation, clinical chemistry, and urinalysis test results not deviating from the normal range to a clinically relevant extent at screening.
- No clinically significant findings on the physical examination at screening.
- Negative results from urine drug screen at screening.
- Ability to communicate well with the investigator, in the local language, and to understand and comply with the requirements of the study.
- Subject covered by Health Insurance system and/or in compliance with the recommendations of the National Law in force relating to biomedical research.
- If the subject's partner could become pregnant, reliable methods of contraception must be used from the time of the first administration of study medication until 3 months following administration of the last dose of study medication.
Exclusion criteria
- Known allergic reactions or hypersensitivity to any excipient of the drug formulation(s).
- History or clinical evidence of any disease and/or existence of any surgical or medical condition which might interfere with the absorption, distribution, metabolism or excretion of the study drug.
- Previous history of fainting, collapse, syncope, orthostatic hypotension, or vasovagal reactions.
- Documented history of chronic liver or gall bladder disease.
- Documented history of hemolytic anemia.
- Veins unsuitable for intravenous puncture on either arm (e.g., veins that are difficult to locate, access, or puncture, veins with a tendency to rupture during or after puncture).
- Previous exposure to the study medication.
- Treatment with another investigational drug within 3 months prior to screening or participation in more than four investigational drug studies within the 12 months prior to screening.
- Subject in the exclusion period of a previous clinical study.
- Subject who had received more than 4,500 Euros as indemnities for his participation in a biomedical research within the 12 last months, including the indemnities for the present study.
- History or clinical evidence of alcoholism or drug abuse within the 3-year period prior to screening.
- Excessive caffeine consumption, defined as 800 mg or more per day at screening.
- Smoking within 3 months prior to screening and inability to refrain from smoking during the course of the study.
- Previous treatment with any prescribed or over-the-counter medications (including herbal medicines such as St. John's Wort) within 2 weeks prior to first study drug administration.
- Loss of 250 mL or more of blood within 3 months prior to screening.
- Positive results from the hepatitis (hepatitis B and C) serology, except for vaccinated subjects.
- Positive results from human immunodeficiency virus serology at screening.
- Any circumstances or conditions, which, in the opinion of the investigator, may affect full participation in the study or compliance with the protocol.
- Legal incapacity or limited legal capacity at screening.
Trial design
Primary purpose
Other
Allocation
Randomized
Interventional model
Parallel Assignment
Masking
Triple Blind
40 participants in 6 patient groups
Group 1
Experimental group
Description:
A single oral dose of 10 mg ACT-451840 or placebo to be administered to subjects in the fasted state. Six subjects are to receive ACT-451840 and 2 subjects to receive matching placebo.
Treatment:
Drug: Placebo
Drug: ACT-451840 10 mg
Group 2
Experimental group
Description:
A single oral dose of 50 mg ACT-451840 or placebo to be administered to subjects in the fasted state. Six subjects are to receive ACT-451840 and 2 subjects to receive matching placebo. If indicated by the pharmacokinetic data obtained in the preceding groups and if not previously performed, a food effect investigation will be conducted after a washout period of at least 7 days. A dose of 50 mg ACT-451840 or placebo is to be administered to subjects in the fed state, followed by the second observation period of 4 days. Six subjects who received ACT-451810 in the fasted state are to receive ACT-451840 in the fed state and 2 subjects who received placebo in the fasted state to receive matching placebo in the fed state.
Treatment:
Drug: Placebo
Drug: ACT-451840 50 mg
Group 3
Experimental group
Description:
A single oral dose of 200 mg ACT-451840 or placebo to be administered to subjects in the fasted state. Six subjects are to receive ACT-451840 and 2 subjects to receive matching placebo. If indicated by the pharmacokinetic data obtained in the preceding groups and if not previously performed, a food effect investigation will be conducted after a washout period of at least 7 days. A dose of 200 mg ACT-451840 or placebo is to be administered to subjects in the fed state, followed by the second observation period of 4 days. Six subjects who received ACT-451810 in the fasted state are to receive ACT-451840 in the fed state and 2 subjects who received placebo in the fasted state to receive matching placebo in the fed state.
Treatment:
Drug: Placebo
Drug: ACT-451840 200 mg
Group 4
Experimental group
Description:
A single dose of 500 mg ACT-451840 or placebo to be administered to subjects in the fasted state, followed by an observation period of 4 days. If indicated by the pharmacokinetic data obtained in the preceding groups and if not previously performed, a food effect investigation will be conducted after a washout period of at least 7 days. A dose of 500 mg ACT-451840 or placebo is to be administered to subjects in the fed state, followed by the second observation period of 4 days. Six subjects who received ACT-451810 in the fasted state are to receive ACT-451840 in the fed state and 2 subjects who received placebo in the fasted state to receive matching placebo in the fed state.
Treatment:
Drug: Placebo
Drug: ACT-451840 500 mg
Group 5
Experimental group
Description:
A single oral dose of 1000 mg ACT-451840 or placebo to be administered to subjects in the fasted state. Six subjects are to receive ACT-451840 and 2 subjects to receive matching placebo. If indicated by the pharmacokinetic data obtained in the preceding groups and if not previously performed, a food effect investigation will be conducted after a washout period of at least 7 days. A dose of 1000 mg ACT-451840 or placebo is to be administered to subjects in the fed state, followed by the second observation period of 4 days. Six subjects who received ACT-451810 in the fasted state are to receive ACT-451840 in the fed state and 2 subjects who received placebo in the fasted state to receive matching placebo in the fed state.
Treatment:
Drug: ACT-451840 1000 mg
Drug: Placebo
Group 6
Experimental group
Description:
A single oral dose of ACT-451840 or placebo to be administered to subjects in the fed state. Six subjects are to receive ACT-451840 and 2 subjects to receive matching placebo. The dose of ACT-451840 to be determined on the basis of the pharmacokinetic results for the previous groups
Treatment:
Drug: Placebo
Drug: ACT-451840 (Dose to be determined)
Trial contacts and locations
1
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Data sourced from clinicaltrials.gov
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