Mass Balance, Pharmacokinetics, and Metabolism of 14C-lab... | NCT02126956

NCT02126956

Protocol Section

Identification Module

Results Section

No data available

No data is available for this block.

Annotation Section

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No data is available for this block.

Document Section

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No data is available for this block.

Derived Section

Miscellaneous Info Module

Status Module

Arms/Interventions Module

Label	Type	Description	Intervention Names
ACT-128800	Experimental	Subjects received a single oral dose of 40 mg 14C-labeled ACT-128800 (one capsule)	Drug: ACT-128800

Interventions

Name	Type	Description	Arm Group Labels	Other Names
ACT-128800	Drug	ACT-128800 was supplied as a powder mix in hard gelatin capsules for oral administration. The capsules contained a co-precipitated mixture of non-radiolabeled and 14C-labeled ACT-128800 formulated at a dose strength of 40 mg with a maximum radioactive content of 102 μCi (3.79 MBq).

Outcomes Module

Primary Outcomes

Measure	Description	Time Frame
Cumulative recovery of total radioactivity expressed as a percentage of the administered dose (mass balance) in the urine	On Day 1, immediately prior to the intake of study drug, subjects were instructed to empty their bladders. Thereafter, following drug intake all urine produced was collected for 10 days up to Day 11 (morning). Following administration of 14C-ACT-128800, urine samples were collected in three consecutive 8-hour intervals, from 0-8 h, 8-16 h, and 16-24 h. From Day 2 to Day 10 (inclusive), urine samples were collected at 24-hour intervals. In case of an extended observation period, urine samples were also collected at 24-hour intervals. The total amount of radioactivity was measured using a liquid scintillation counter.	Up to end of study, approximately 240 hours
Cumulative recovery of total radioactivity expressed as a percentage of the administered dose (mass balance) in the faeces	Between Day -3 and Day -1, a baseline faeces sample was collected in a light-protected polypropylene box from each subject. From Day 1 (post-dose) to Day 10 (inclusive), all faeces samples and the toilet paper were collected in pre-weighed, light-protected polypropylene boxes. Each faeces sample was collected in a separate box and weighed. The weight of the sample and the time of collection were recorded. All faecal samples were frozen as soon as possible and stored in an upright position at -70 °C or below.The total amount of radioactivity was measured using a liquid scintillation counter.	Up to end of study, approximately 240 hours

Secondary Outcomes

Measure	Description	Time Frame
Maximum concentration (Cmax) of 14C-radioactivity in whole blood	Blood samples were collected from an antecubital vein by direct venipuncture or via an intravenous catheter at various time points up to the end of study. An aliquot of 2.0 mL was used for measurement of radioactivity. The amount of radioactivity was measured using a liquid scintillation counter. The measured radioactivity was used to directly obtain Cmax.

Eligibility Module

Eligibility Criteria

Inclusion Criteria:

Signed informed consent prior to any study-mandated procedure.
Male and aged between 45 and 65 years (inclusive) at screening.
No clinically significant findings on physical examination performed at screening.
Body mass index (BMI) between 18-28 kg/m^2 (inclusive) at screening.
Systolic blood pressure 100-145 mmHg, diastolic blood pressure 50-90 mmHg, and heart rate 55-90 bpm (inclusive), measured on the leading arm, after 5 minutes in the supine position at screening. These criteria should also be met before the administration of the first dose.
12-lead electrocardiogram without clinically relevant abnormalities at screening.
Clinical chemistry, hematology, and urinalysis results not deviating from the normal range to a clinically relevant extent 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.

Exclusion Criteria:

Known hypersensitivity to any excipients of the drug formulation.
Treatment with another investigational drug within the 3 months prior to screening.
History or clinical evidence of alcoholism or drug abuse within the 3-year period prior to screening.
Excessive caffeine consumption, defined as ≥ 800 mg per day at screening.
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.
Smoking within the 3 months prior to screening.
Any immunosuppressive treatment within 6 weeks before study drug administration.
Previous treatment with any prescribed or over-the-counter medications (including herbal medicines such as St John's Wort) within 2 weeks prior to screening.
Loss of 250 mL or more of blood within the 3 months prior to screening.
Lymphopenia (< 1,100 lymphocytes/μL).
Viral, fungal, bacterial or protozoal infection within 4 weeks before study drug administration.
Positive hepatitis B or hepatitis C serology, except for vaccinated subjects, at screening.
Positive 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.
Exposure to artificial ionizing radiation (e.g., X-ray, thyroid scan, study with radiolabeled compound) in the 12-month period before screening.
A history of clinically relevant constipation (defined as lasting more than 3 days) in the 4-week period before screening.