safety, tolerability, pharmacokinetics, and pharmacodynamics of act-451840 in healthy subjects (part a)

Conditions: Healthy

Summary: 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.


Eligibility criteria:
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.

Keywords: act-451840 safety tolerability pharmacokinetics